bluuebunny/crossref_metadata_2025 huggingface dataset:
ChemInform Abstract: Selective Formation of 1,5‐Substituted Sulfonyl Triazoles Using Acetylides and Sulfonyl Azides.
Authors: Meza‐Avina Maria Elena , Patel Mudita Kishor , Lee Cylivia B. , Dietz Thomas J. , Croatt Mitchell P.
Published: September 2011

When being purified by silica gel chromatography, isomerization of the products to 1,4‐triazoles partially occurs.
ChemInform Abstract: Unprecedented Cu‐Catalyzed Coupling of Internal 1,3‐Diynes with Azides: One‐Pot Tandem Cyclizations Involving 1,3‐Dipolar Cycloaddition and Carbocyclization Furnishing Naphthotriazoles.
Authors: Mandadapu Anil K. , Sharma Sudhir K. , Gupta Sahaj , Krishna Deevi G. Venkata , Kundu Bijoy
Published: September 2011

A variety of target compounds is prepared from aromatic symmetrical internal diynes and aromatic and aliphatic azides.
ChemInform Abstract: Highly Stereoselective Broensted Acid Catalyzed Synthesis of Spirooxindole Pyrans.
Authors: Wang Jingqi , Crane Erika A. , Scheidt Karl A.
Published: September 2011

Prins‐type cyclization of β‐hydroxy dioxinones and isatin dimethylacetals is used to construct the title skeletons with complete diastereoselectivity.
ChemInform Abstract: A Novel Organozinc Reagent 4‐Coumarinylzinc Bromide; Preparation and Application in the Synthesis of 4‐Substituted Coumarin Derivatives.
Authors: Rieke Reuben D. , Kim Seung‐Hoi
Published: September 2011

A novel organozinc reagent (I) is prepared by the direct oxidative addition of active zinc to 4‐bromocoumarin.
ChemInform Abstract: An Efficient One‐Pot Synthesis of Flavones.
Authors: Chee Chin Fei , Buckle Michael J. C. , Rahman Noorsaadah Abd.
Published: September 2011

Flavones are prepared from the corresponding hydroxy‐acetophenones (I) and aroyl chlorides (II) to afford a good yield of flavones (III) and a smaller amount of 3‐aroylflavones (IV).
ChemInform Abstract: Synthesis of Functionalized CF3‐Containing Heterocycles via [2,3]‐Sigmatropic Rearrangement and Sequential Catalytic Carbocyclization.
Authors: Vorobyeva Daria V. , Mailyan Artur K. , Peregudov Alexander S. , Karimova Natalia M. , Vasilyeva Tamara P. , Bushmarinov Ivan S. , Bruneau Christian , Dixneuf Pierre H. , Osipov Sergey N.
Published: September 2011

Copper‐catalyzed tandem ylide formation—[2,3]‐sigmatropic rearrangement of CF3‐containing diazo compounds (II) with amines and sulfides containing two allyl and/or propargyl groups, e.g. (I), (V), (IX) or (XIII), affords the corresponding dienes, enynes or allenynes.
ChemInform Abstract: Cerium Ammonium Nitrate Catalyzed Multicomponent Reaction for Efficient Synthesis of Functionalized Tetrahydropyridines.
Authors: Wang Hong‐Juan , Mo Li‐Ping , Zhang Zhan‐Hui
Published: September 2011

The reaction proceeds under mild conditions and tolerates a wide range of substrates.
ChemInform Abstract: Novel Synthetic Methodologies. Part 206. Molybdenum‐ and Tungsten‐Based Coordination Polymers as Catalysts for an Efficient and Rapid Synthesis of Hexahydro‐5‐oxoquinoline‐3‐carboxylates and 1,4‐Dihydropyridine‐3,5‐dicarboxylates.
Authors: Das Biswanath , Srilatha Malampati , Veeranjaneyulu Boyapati , Kanth Boddu Shashi
Published: September 2011

Almost equally active is the respective tungsten‐based catalyst.
ChemInform Abstract: α‐Dimethylaminomethylenation‐Induced Houben—Hoesch‐Type Cyclization of Cyanoacetanilides: A Practical Synthesis of 3‐Formyl‐4‐hydroxyquinolin‐2(1H)‐ones.
Authors: Kobayashi Yusuke , Nakatani Terue , Tanaka Rie , Okada Mari , Torii Eri , Harayama Takashi , Kimachi Tetsutaro
Published: September 2011

The triflic acid‐mediated cyclization of cyanoacetanilides (I) in DMF to give title formylquinolinones (III) is studied.
ChemInform Abstract: Stable Azomethine Imines Having a 3,4‐Dihydroisoquinoline Fragment and Their Cycloaddition to N‐Arylmaleimides.
Authors: Koptelov Yu. B. , Saik S. P. , Molchanov A. P.
Published: September 2011

1,3‐Dipolar cycloaddition of N‐arylmaleimides (IV) to azomethine imines (III) leads to cis‐ and trans‐adducts (V) and (VI) in ratios depending on the ortho substituent in the aryl moiety of (IV).
ChemInform Abstract: Synthesis and Antibacterial Activity of Some Novel Pyrazolopyridine Derivatives.
Authors: Panda N. , Karmakar S. , Jena A. K.
Published: September 2011

A variety of novel pyrazolopyridine derivatives are synthesized by Friedlaender condensation of aldehyde (VII) with active methylene compounds.
ChemInform Abstract: Diastereoselective Intramolecular Friedel—Crafts Alkylation of Tetralins.
Authors: Liebert Clemence , Brinks Marion K. , Capacci Andrew G. , Fleming Matthew J. , Lautens Mark
Published: September 2011

A wide range of cis‐hexahydrobenzophenanthridine‐derived cyclic compounds is prepared in a mild reaction from the corresponding chiral tetralin substrates with retention of optical purity.
ChemInform Abstract: An Efficient Synthesis of 1‐Thia‐5‐azaspiro[5.5]undec‐2‐ene and Its Recyclization to 1,5‐Diazaspiro[5.5]undec‐2‐ene and/or Spiro‐Thieno[2,3‐d]pyrimidin‐4(1H)‐one Derivatives.
Authors: Shaker Raafat M. , Hamoda Asmaa , Ibrahim Yusria R. , El‐Shaieb Kamal M. , Abdel‐Latif Fathy F.
Published: September 2011

Spiro compound (III) is used as key intermediate for the synthesis of a series of derivatives.
ChemInform Abstract: New Efficient Synthesis of 2,3,4‐Trisubstituted 3,4‐Dihydroquinazolines by a Ugi 4CC/Staudinger/Aza‐Wittig Sequence.
Authors: Zhong Ying , Wang Long , Ding Ming‐Wu
Published: September 2011

The azide products are transformed at room temperature by the Staudinger reaction into intermediate iminophosphoranes which undergo an aza‐Wittig reaction under to give the desired quinazolines.
ChemInform Abstract: Thermal Solvent‐Free Synthesis of Novel Pyrazolyl Chalcones and Pyrazolines as Potential Antimicrobial Agents.
Authors: Siddiqui Zeba N. , Musthafa T. N. Mohammed , Ahmad Anis , Khan Asad U.
Published: September 2011

Simple thermal heating under neat conditions gives access to new chalcones (III) which are then converted to the corresponding pyrazolines (IV) in a solvent‐free reaction.
ChemInform Abstract: Microwave‐Assisted Synthesis, Crystal Structure of Pyrazolo[1,5‐a]pyrazin‐4(5H)‐ones and Their Selective Effects on Lung Cancer Cells.
Authors: Liu Ning , Zhang Jin‐Hua , Zhao Bao‐Xiang , Zhao Jing , Su Le , Dong Wen‐Liang , Zhang Shang‐Li , Miao JunYing
Published: September 2011

A facile microwave‐assisted route to pyrazolopyrazinones (III) (12 examples) is given.
ChemInform Abstract: Zn[(L)proline]2 in Water: A New Easily Accessible and Recyclable Catalytic System for the Synthesis of Pyrazoles.
Authors: Kidwai Mazaahir , Jain Arti , Poddar Roona
Published: September 2011

A variety of pyrazoles and diazepines is prepared from 1,3‐dicarbonyl compounds and hydrazine, hydrazides, ortho‐phenylenediamine and 4,5‐diaminophthalonitrile.
ChemInform Abstract: A Facile Method to Construct Cyclic α,α‐Difluoromethylenephosphonate — A Novel Cyclic Phosphate Mimic.
Authors: Lin Yun , Liu Jin‐Tao
Published: September 2011

Cyclic α,α‐difluoromethylenephosphonates of type (II) and (V) are prepared by halogen‐induced intramolecular cyclization of (I) or (IV).
ChemInform Abstract: Palladium‐Catalyzed Cross‐Coupling of H‐Phosphinate Esters with Chloroarenes.
Authors: Deal Eric L. , Petit Christelle , Montchamp Jean‐Luc
Published: September 2011

A wide range of aromatic and heteroaromatic phosphinates is prepared.
ChemInform Abstract: Synthesis of Aryl(ferrocenyl)methanols via an Enantioselective Addition of Arylboronic Acids.
Authors: Tisovsky Pavol , Meciarova Maria , Sebesta Radovan
Published: September 2011

The reaction proceeds via microwave‐assisted formation of zinc reagents and is catalyzed by ferrocenyl oxazolinyl alcohol.
ChemInform Abstract: Synthesis and Antitumor Activity of Ring A‐Modified Glycyrrhetinic Acid Derivatives.
Authors: Csuk Rene , Schwarz Stefan , Siewert Bianka , Kluge Ralph , Stroehl Dieter
Published: September 2011

A series of derivatives of glycyrrhetinic acid (Ia) with altered lipophilicity in ring A are prepared and their apoptotic activities are discussed.
ChemInform Abstract: Antifibrotic Constituents of Alnus firma on Hepatic Stellate Cells.
Authors: Lee Mina , Lee Mi Kyeong , Kim Young Choong , Sung Sang Hyun
Published: September 2011

Bioactivity‐guided fractionation leads to the isolation of a new triterpenoid characterized as lup‐20(29)en‐2,28‐diol‐3‐yl caffeate (I) together with 12 known diarylheptanoids.
ChemInform Abstract: In vitro and in vivo Anticancer Activity Evaluation of Ursolic Acid Derivatives.
Authors: Shao Jing‐Wei , Dai Yong‐Chao , Xue Jin‐Ping , Wang Ji‐Chuang , Lin Feng‐Ping , Guo Yang‐Hao
Published: September 2011

Twentythree ursolic acid derivatives including ten novel compounds are synthesized by modification of the C‐3 and C‐28 positions.
ChemInform Abstract: Cytotoxic and PPARs Transcriptional Activities of Sterols from the Vietnamese Soft Coral Lobophytum laevigatum.
Authors: Kim Young Ho , et al. et al.
Published: September 2011

A new unusual sterol, named lobophytosterol (I), and five known metabolites are isolated from the methanol extract of the soft coral Lobophytum laevigatum.
ChemInform Abstract: Penicisteroids A and B, Antifungal and Cytotoxic Polyoxygenated Steroids from the Marine Alga‐Derived Endophytic Fungus Penicillium chrysogenum QEN‐24S.
Authors: Gao Shu‐Shan , Li Xiao‐Ming , Li Chun‐Shun , Proksch Peter , Wang Bin‐Gui
Published: September 2011

Two new polyoxygenated steroids, named penicisteroids A (I) and B (II), are obtained from the culture extract of Penicillium chrysogenum QEN‐24S, an endophytic fungus isolated from an unidentified marine red algal species.
ChemInform Abstract: Biological Evaluation of 3′‐O‐Alkylated Analogues of Salacinol, the Role of Hydrophobic Alkyl Group at 3′ Position in the Side Chain on the α‐Glucosidase Inhibitory Activity.
Authors: Tanabe Genzoh , Otani Tetsu , Cong Wenying , Minematsu Toshie , Ninomiya Kiyofumi , Yoshikawa Masayuki , Muraoka Osamu
Published: September 2011

Four hydrophobically modified analogues (I) of the naturally occurring α‐glucosidase inhibitor salacinol are prepared and evaluated for their inhibitory activity.
ChemInform Abstract: Synthesis of Substituted Indolizino[8,7‐b]indoles from Harmine and Their Biological Activity.
Authors: Nurmaganbetov Zh. S. , Shultz E. E. , Chernov S. V. , Turmukhambetov A. Zh. , Seydakhmetova R. B. , Shakirov M. M. , Tolstikov G. A. , Adekenov S. M.
Published: September 2011

Title compounds [(VI), (VIII), and (X)] are synthesized starting from harmine (I) via quaternized derivatives (V).
ChemInform Abstract: Asymmetric Synthesis of Stagonolide‐D and Stagonolide‐G.
Authors: Mahapatra Tridib , Das Tapas , Nanda Samik
Published: September 2011

Stagonolide‐D (VII) is obtained via HWE‐olefination of aldehyde (I), selective reduction of ester (III), Sharpless asymmetric epoxidation of alkene (IV), and ring‐closing metathesis of diene (VI) as key steps.
ChemInform Abstract: Synthesis and Biological Evaluation of 4‐Nitro‐Substituted 1,3‐Diaryltriazenes as a Novel Class of Potent Antitumor Agents.
Authors: Osmak Maja , et al. et al.
Published: September 2011

p‐Nitro‐substituted 1,3‐diaryltriazenes with two additional electron‐withdrawing groups at their ortho position are highly cytotoxic.
ChemInform Abstract: Soft Mechanochemical Synthesis of Materials for Lithium‐Ion Batteries: Principles and Applications
Authors: Kosova N. V.
Published: September 2011

Review: 46 refs.
ChemInform Abstract: Polymorphous Transformations of Nanometric Iron(III) Oxide: A Review
Authors: Machala Libor , Tucek Jiri , Zboril Radek
Published: September 2011

Review: 165 refs.
ChemInform Abstract: X‐Ray Diffraction Structure Diagnostics of Nanomaterials
Authors: Moroz E. M.
Published: September 2011

Review: 124 refs.
ChemInform Abstract: Synthesis and Applications of Magnetic‐Metal Nanotubes
Authors: Nakagawa Masaru , Oda Hirokazu , Kobayashi Kei
Published: September 2011

Review: 56 refs.
ChemInform Abstract: Preparation of Crystalline CrVO4 Catalyst by Soft Chemistry Technique and Application for Vapor‐Phase Oxidation of Picolines
Authors: Shishido Tetsuya
Published: September 2011

Review: 56 refs.
ChemInform Abstract: Porphyrin Complexes of the Period 6 Main Group and Late Transition Metals
Authors: Lemon Christopher M. , Brothers Penelope J. , Boitrel Bernard
Published: September 2011

Review: 110 refs.
ChemInform Abstract: Ruthenium Complexes Containing Iminophosphorane Ligands: Synthesis, Structure, Reactivity and Applications
Authors: Cadierno Victorio , Garcia‐Alvarez Joaquin
Published: September 2011

Review: 173 refs.
ChemInform Abstract: Chemistry and Applications of Organotin(iv) Complexes of Schiff Bases
Authors: Nath Mala , Saini Pramendra K.
Published: September 2011

Review: 159 refs.
ChemInform Abstract: Surface‐Initiated Polymerization of Conjugated Polymers
Authors: Marshall Nicholas , Sontag S. Kyle , Locklin Jason
Published: September 2011

Review: 61 refs.
ChemInform Abstract: Carbene Insertion into Transition Metal—Carbon Bonds: A New Tool for Catalytic C—C Bond Formation.
Authors: Franssen Nicole M. G. , Walters Annemarie J. C. , Reek Joost N. H. , de Bruin Bas
Published: September 2011

Review: 92 refs.
ChemInform Abstract: Current Methods for Asymmetric Halogenation of Olefins
Authors: Castellanos Alejandro , Fletcher Stephen P.
Published: September 2011

Review: stoichiometric and catalytic methods; 78 refs.
ChemInform Abstract: Platinum Metals in the Catalytic Asymmetric Isomerization of Allylic Alcohols
Authors: Mantilli Luca , Mazet Clement
Published: September 2011

Review: 28 refs.
ChemInform Abstract: Chemical Modification of Antifungal Polyene Macrolide Antibiotics
Authors: Solovieva S. E. , Olsufyeva E. N. , Preobrazhenskaya M. N.
Published: September 2011

Review: 62 refs.
ChemInform Abstract: Studies on Anticonvulsant Agents. Achievements and Prospects
Authors: Pandey Sh. , Shukla Sh. , Pandey D. , Srivastava R. S.
Published: September 2011

Review: 69 refs.
ChemInform Abstract: Application of Click Chemistry on Preparation of Separation Materials for Liquid Chromatography
Authors: Chu Changhu , Liu Renhua
Published: September 2011

Review: 52 refs.
ChemInform Abstract: Cyclodextrin‐Based Inclusion Complexation Bridging Supramolecular Chemistry and Macromolecular Self‐Assembly
Authors: Chen Guosong , Jiang Ming
Published: September 2011

Review: 52 refs.
ChemInform Abstract: The Effects of Cyclodextrins on the Conformation of Proteins
Authors: Yamamoto Tatsuyuki , Yoshikiyo Keisuke
Published: September 2011

Review: 42 refs.
ChemInform Abstract: Advances in Synthetic Approach to and Antifungal Activity of Triazoles
Authors: Shalini Kumari , Kumar Nitin , Drabu Sushma , Sharma Pramod Kumar
Published: September 2011

Review: 75 refs.
ChemInform Abstract: Crystalline Molecular Flasks
Authors: Inokuma Yasuhide , Kawano Masaki , Fujita Makoto
Published: September 2011

Review: 62 refs.
ChemInform Abstract: Biomimetic Oxidation of Alkanes
Authors: Karasevich E. I.
Published: September 2011

Review: 133 refs.
ChemInform Abstract: Conductive Polymers: Materials and Applications
Authors: Supaphol Pitt , Aramwit Pornanong , Sangsanoh Pakakrong , Changsarn Sutheerat , Chuangchote Surawut , de Villiers Melgardt M.
Published: September 2011

Review: 101 refs.
ChemInform Abstract: Advances in Bonding Plastics
Authors: Jialanella G. L.
Published: September 2011

Review: 59 refs.
ChemInform Abstract: Solid‐State Nuclear Magnetic Resonance Investigations of the Nature, Property, and Activity of Acid Sites on Solid Catalysts
Authors: Jiang Yijiao , Huang Jun , Dai Weili , Hunger Michael
Published: September 2011

Review: 214 refs.
ChemInform Abstract: EPR Investigations of Organic Non‐Covalent Assemblies with Spin Labels and Spin Probes
Authors: Lucarini Marco , Mezzina Elisabetta
Published: September 2011

Review: 71 refs.
Review on Portable Energy Systems: From Electrochemical Systems to Energy Harvesting
Authors: Krewer Ulrike
Published: September 2011

Portable Energiesysteme stellen ortsunabhängig elektrische Energie zur Verfügung. Eingesetzt werden bisher hauptsächlich elektrochemische Energiespeicher, üblicherweise Batterien. Diese sind jedoch nur bedingt für netzferne Anwendungen mit höherer Laufzeit oder höherem Energiebedarf geeignet; hier werden Energiewandler wie Brennstoffzellen, Mikroturbinen und Energy‐Harvesting‐Technologien eingesetzt. Dieser Übersichtsartikel stellt alle Technologien aus verfahrenstechnischer Sicht dar, vergleicht die Technologien und gibt Einblicke in den Stand der Forschung und zukünftige Herausforderungen.
Reduction of Hydrocarbon Emissions in Solar Cell Fabrication – A Life Cylce Assessment
Authors: Hottenroth Heidi , Schottler Martin , Schmidt Mario
Published: September 2011

Mit Hilfe einer Ökobilanz werden verschiedene technologische Varianten zur Minderung von Kohlenwasserstoffemissionen bei der Solarzellenfertigung untersucht. Hierbei verursachen die Verbrennungsverfahren deutlich mehr potenzielle Umweltwirkungen als die Kondensation oder der Biofilter. Beim Vergleich der Minderungstechnologien mit der direkten Abgabe der unbehandelten Abluft an die Umbebung zeigt sich, dass durch die untersuchten Behandlungsverfahren die beabsichtigte Verminderung von Gesundheitsbelastungen überkompensiert wird. Das Ziel der Richtlinie zur integrierten Vermeidung und Verminderung von Umweltverschmutzung – den Schutz der Umwelt insgesamt zu gewährleisten – wird somit durch diese Verfahren nicht erfüllt.
The permeability of wood‐chip beds: The effect of compressibility
Authors: Alaqqad M. , Bennington C. P. J. , Martinez D. M.
Published: September 2011

In this work, we present a methodology to characterise the permeability of a compressible bed of wood chips under mechanical load. We show that under the limiting condition of when the mechanical compression is large in comparison to hydraulic pressure the equations of motion can be linearised and solved to produce an expression approximating the variation in porosity along the length of the bed. We show how this may be used, in conjunction with multiple linear regression to estimate permeability of the bed. In the experimental portion of the work we measure the permeability of a bed of hemlock wood chips at three different kappa numbers κ, and compacted to three different mechanical loads, i.e. compaction pressures pc. The usefulness of these estimates was then tested by predicting the pressure drop versus flow relationship for conditions outside the range of the linearised solution; the equations of motion were solved numerically with knowledge of the measured permeability. Good agreement was obtained. After accounting for compressibility effects, we find that our correlation has lower flow resistances than the literature correlations. © 2011 Canadian Society for Chemical Engineering
Synthesis of New 2‐Phenylpyrano[3,2‐b]phenothiazin‐4(6H)‐one Derivatives
Authors: Bansode Tanaji N. , Meshram Gangadhar A.
Published: September 2011

A new synthesis of 2‐phenylpyrano[3,2‐b]phenothiazin‐4(6H)‐one derivatives was reported. First 2,10‐diacetyl‐3‐hydroxyphenothiazine (2) was converted into their benzoyloxy esters (3a–3j) using different aromatic carboxylic acids in the presence of phosphorous oxychloride in pyridine. Benzoyloxy esters were converted into their 1,3‐diones (4a–4j) by using dry KOH in pyridine via Baker‐Venkataraman transformation reaction. The 1,3‐diones thus obtained were cyclised to pyranophenothiazines (5a–5j) by refluxing in an acetic acid/HCl mixture.
Acquired Long QT Interval: A Case Series of Multifactorial QT Prolongation
Authors: Digby Geneviève C. , Pérez Riera Andrés Ricardo , Barbosa Barros Raimundo , Simpson Christopher S. , Redfearn Damian P. , Methot Michelle , Femenía Francisco , Baranchuk Adrian
Published: September 2011

Background:

Acquired long QT (LQT) interval is thought to be a consequence of drug therapy and electrolyte disturbances.

Hypothesis:

We characterize the potential effects of polypharmacy in a case series of acquired LQT and torsades de pointes (TdP) in order to determine whether multiple risk factors play a role in the development of LQT.

Methods:

The case series consisted of 11 patients presenting to 4 tertiary care hospitals with LQT and ≥2 risk factors for developing LQT. Clinical characteristics, medications, electrolyte disturbances, and course in hospital were analyzed.

Results:

Mean age was 49.1 ± 5.8 years. Eight patients were female. Four had hypertension, 1 had a history of dilated cardiomyopathy, and 1 patient demonstrated complete atrioventricular block. Average QTc interval at presentation was 633.8 ± 29.2 ms. Nine patients developed TdP. In 3, LQT was not initially detected and amiodarone was administered, followed by development of TdP. Patients were taking an average of 2.8 ± 0.3 QT‐prolonging medications—an antidepressant in 6 cases and a diuretic in 8 cases. All patients had an electrolyte abnormality; 8 patients presented with severe hypokalemia (<3.0 mmol/L). Average serum potassium and magnesium were 2.82 ± 0.10 mmol/L and 0.75 ± 0.03 mmol/L, respectively. There were no deaths.

Conclusions:

This case series highlights the risks of polypharmacy in the development of LQT and TdP. It illustrates the importance of early detection of LQT in patients with multiple risk factors in ensuring appropriate treatment. © 2011 Wiley Periodicals, Inc.

The authors have no funding, financial relationships, or conflicts of interest to disclose.
Structure–Activity Relationship for the First‐in‐Class Clinical Steroid Sulfatase Inhibitor Irosustat (STX64, BN83495)
Authors: Woo L. W. Lawrence , Ganeshapillai Dharshini , Thomas Mark P. , Sutcliffe Oliver B. , Malini Bindu , Mahon Mary F. , Purohit Atul , Potter Barry V. L.
Published: September 2011

Structure–activity relationship studies were conducted on Irosustat (STX64, BN83495), the first steroid sulfatase (STS) inhibitor to enter diverse clinical trials for patients with advanced hormone‐dependent cancer. The size of its aliphatic ring was expanded; its sulfamate group was N,N‐dimethylated, relocated to another position and flanked by an adjacent methoxy group; and series of quinolin‐2(1H)‐one and quinoline derivatives of Irosustat were explored. The STS inhibitory activities of the synthesised compounds were assessed in a preparation of JEG‐3 cells. Stepwise enlargement of the aliphatic ring from 7 to 11 members increases potency, although a further increase in ring size is detrimental. The best STS inhibitors in vitro had IC50 values between 0.015 and 0.025 nM. Other modifications made to Irosustat were found to either abolish or significantly weaken its activity. An azomethine adduct of Irosustat with N,N‐dimethylformamide (DMF) was isolated, and crystal structures of Irosustat and this adduct were determined. Docking studies were conducted to explore the potential interactions between compounds and the active site of STS, and suggest a sulfamoyl group transfer to formylglycine 75 during the inactivation mechanism.
N‐[2‐Methyl‐5‐(triazol‐1‐yl)phenyl]pyrimidin‐2‐amine as a Scaffold for the Synthesis of Inhibitors of Bcr‐Abl
Authors: Arioli Federica , Borrelli Stella , Colombo Francesco , Falchi Federico , Filippi Irene , Crespan Emmanuele , Naldini Antonella , Scalia Giusy , Silvani Alessandra , Maga Giovanni , Carraro Fabio , Botta Maurizio , Passarella Daniele
Published: September 2011

N‐[2‐Methyl‐5‐(triazol‐1‐yl)phenyl]pyrimidin‐2‐amine derivatives were synthesized and evaluated in vitro for their potential use as inhibitors of Bcr‐Abl. The design is based on the bioisosterism between the 1,2,3‐triazole ring and the amide group. The synthesis involves a copper(I)‐catalyzed azide–alkyne cycloaddition (CuAAC) as the key step, with the exclusive production of anti‐(1,4)‐triazole derivatives. One of the compounds obtained shows general activity similar to that of imatinib; in particular, it was observed to be more effective in decreasing the fundamental function of cdc25A phosphatases in the K‐562 cell line.
The impact of July hospital admission on outcome after surgery for spinal metastases at academic medical centers in the United States, 2005 to 2008
Authors: Dasenbrock Hormuzdiyar H. , Clarke Michelle J. , Thompson Richard E. , Gokaslan Ziya L. , Bydon Ali
Published: September 2011

BACKGROUND:

Despite widespread belief that patients admitted to teaching hospitals in July—the beginning of the academic year—have inferior outcomes, there has been little evidence to support the existence of the July phenomenon. Moreover, the impact of July admission on the outcomes after surgery for spinal metastases has not been investigated.

METHODS:

Data from the Nationwide Inpatient Sample (2005‐2008) were retrospectively extracted. Patients who underwent surgery for metastatic spinal disease and were admitted to a teaching hospital were included. Multivariate logistic regression was conducted to calculate the odds of in‐hospital death, the occurrence of an intraoperative complication, and the development of a postoperative complication depending on whether admission was in July or between August and June. All analyses were adjusted for differences in patient age, sex, comorbidities, primary tumor histology, visceral metastases, myelopathy, insurance status, hospital volume, and admission type.

RESULTS:

A total of 2920 admissions were evaluated. In‐hospital mortality was higher in July compared with between August and June—7.5% versus 4.2%. The adjusted odds of in‐hospital death were significantly higher for patients admitted in July (odds ratio [OR], 1.81; 95% confidence interval [CI], 1.13‐2.91; P = .01). Patients admitted in July were significantly more likely to develop an intraoperative complication (OR, 2.11; 95% CI, 1.41‐3.17; P < .001), but not a postoperative complication (OR, 1.08; 95% CI, 0.81‐1.45; P = .60).

CONCLUSIONS:

In this nationwide study based on an administrative database, patients undergoing surgery for metastatic spinal disease at teaching hospitals in July had higher rates of in‐hospital mortality and intraoperative complications. Cancer 2012;. © 2011 American Cancer Society.
Randomized controlled trial of acitretin versus placebo in patients at high‐risk for basal cell or squamous cell carcinoma of the skin (North Central Cancer Treatment Group Study 969251)
Authors: Kadakia Kunal C. , Barton Debra L. , Loprinzi Charles L. , Sloan Jeff A. , Otley Clark C. , Diekmann Brent B. , Novotny Paul J. , Alberts Steven R. , Limburg Paul J. , Pittelkow Mark R.
Published: September 2011

BACKGROUND:

Chemoprevention with systemic retinoids has demonstrated promise in decreasing the incidence of new primary nonmelanoma skin cancers (NMSCs) in immunocompromised post‐transplantation recipients. There is limited evidence for the use of systemic retinoids in the nontransplantation patient. To the authors' knowledge, this is the first randomized controlled trial to assess the efficacy of acitretin as a chemopreventive agent in nontransplantation patients at high‐risk for NMSC.

METHODS:

The study was designed as a prospective, randomized, double‐blind, placebo‐controlled clinical trial. To test the possible skin cancer‐preventing effect of a 2‐year treatment with acitretin, 70 nontransplantation patients aged ≥18 years who had a history of ≥2 NMSCs within 5 years of trial onset were randomized to receive either placebo or acitretin 25 mg orally 5 days per week. The primary outcome measure was the rate of new NMSC development.

RESULTS:

Seventy patients were randomized to receive either acitretin alone (N = 35) or placebo (N = 35). During the 2‐year treatment period, the patients who received acitretin did not have a statistically significant reduction in the rate of new primary NMSCs (odds ratio, 0.41; 95% confidence interval, 0.15‐1.13; 54% vs 74%; P = .13). However, using the incidence of new NMSC, the time to new NMSC, and total NMSC counts, an umbrella test indicated a significant trend that favored the use of acitretin (chi‐square statistic, 3.94; P = .047). The patients who received acitretin reported significantly more mucositis and skin toxicities compared with the patients who received placebo.

CONCLUSIONS:

Although there was not a statistically significant benefit observed with the use of acitretin, this may have been the result of low statistical power. Cancer 2012;. © 2011 American Cancer Society.
Prognostic value of MYC rearrangement in cases of B‐cell lymphoma, unclassifiable, with features intermediate between diffuse large B‐cell lymphoma and Burkitt lymphoma
Authors: Lin Pei , Dickason Timothy J. , Fayad Luis E. , Lennon Patrick A. , Hu Peter , Garcia Mar , Routbort Mark J. , Miranda Roberto , Wang Xumei , Qiao Wei , Medeiros L. Jeffrey
Published: September 2011

BACKGROUND:

B‐cell lymphoma, Unclassifiable with features intermediate between diffuse large B‐cell lymphoma (DLBCL) and Burkitt lymphoma, for convenience referred to here as unclassifiable B‐cell lymphoma, is a category in the 2008 World Health Organization system used for a group of histologically aggressive neoplasms that are difficult to classify definitively. Currently, there is no established standard therapy for these neoplasms.

METHODS:

The authors assessed MYC status and correlated it with treatment response and outcome in a group of 52 patients with unclassifiable B‐cell lymphoma treated with either a standard DLBCL regimen (R‐CHOP [rituximab plus cyclophosphamide, doxorubicin, vincristine, and prednisolone‐related therapy]) or more intensive regimens, such as R‐hyper‐CVAD (rituximab plus hyperfractionated cyclophosphamide, vincristine, doxorubicin, and dexamethasone alternating with high‐dose methotrexate and cytarabine). The regimens were selected by the treating clinicians based on the overall clinical and pathological findings.

RESULTS:

Thirty (58%) unclassifiable B‐cell lymphomas had MYC abnormalities (MYC+) including 27 with rearrangement, 2 with amplification, and 1 with both. The MYC+ and MYC− groups were similar in their age distribution and International Prognostic Index scores. Progression‐free survival of patients with MYC+ unclassifiable B‐cell lymphoma treated initially with R‐CHOP was significantly worse than patients treated with R‐hyper‐CVAD (P = .0358). In contrast, for the MYC− unclassifiable B‐cell lymphoma group, some patients responded to R‐CHOP, and others were refractory to R‐hyper‐CVAD.

CONCLUSIONS:

MYC aberrations are common in unclassifiable B‐cell lymphoma. The presence of MYC aberrations identifies a patient subset that requires more aggressive therapy than R‐CHOP. In contrast, MYC− unclassifiable B‐cell lymphoma patients responded variably to either R‐CHOP or aggressive therapy, and the latter showed no survival advantage. Cancer 2011;. © 2011 American Cancer Society.
Genetic sequence variants and the development of secondary primary cancers in patients with head and neck cancers
Authors: Azad Abul Kalam , Bairati Isabelle , Samson Elodie , Cheng Dangxiao , Cheng Lu , Mirshams Maryam , Savas Sevtap , Waldron John , Wang Changshu , Goldstein David , Xu Wei , Meyer Francois , Liu Geoffrey
Published: September 2011

BACKGROUND:

Secondary primary cancers (SPCs), a major cause of morbidity and mortality in head and neck cancers (HNCs), are commonly associated with field cancerization. We comprehensively evaluated 23 germline sequence variants (from published literature) in 17 genes from 7 biological pathways associated with the HNC survival. Because cancer prognosis correlates with disease aggressiveness, the factors that determine aggressive disease may influence field cancerization process to favor SPC development. We thus hypothesized that the same sequence variants associated with HNC survival can also be associated with SPC.

METHODS:

Germline DNA from 531 stage I‐II radiation‐treated HNC patients (originally recruited for an alpha‐tocopherol/beta‐carotene placebo‐controlled secondary prevention clinical trial) were genotyped, and analyzed using Cox proportional hazards models, stratified by treatment arm, adjusting for clinical prognostic factors.

RESULTS:

The majority of SPCs were of lung and HNCs. Median follow‐up time was 5 years. SPCs were diagnosed in 21% of patients. The 5‐year SPC‐free survival was 79%. All but 1 evaluated sequence variant were not associated with SPC. There was a strong association of the DNA (cytosine‐5‐)‐methyltransferase 3 beta (DNMT3B) sequence variant, DNMT3B:C149T (rs2424913) with SPC: the adjusted hazard ratio (aHR) for TT versus CC was 2.23 (1.32‐3.78; P = .003), whereas each variant T allele was associated with an aHR of 1.49 (1.15‐1.95; P = .003).

CONCLUSIONS:

A functional sequence variant in DNMT3B is associated with the development of SPCs in HNC early stage patients treated with radiation. Aberrant DNA methylation may be an important modulator of SPC development in at‐risk individuals with HNCs. Cancer 2011;. © 2011 American Cancer Society.
Insulin resistance, central obesity, and risk of colorectal adenomas
Authors: Ortiz Ana Patricia , Thompson Cheryl L. , Chak Amitabh , Berger Nathan A. , Li Li
Published: September 2011

BACKGROUND:

Increasing evidence supports insulin resistance (IR) as the underpinning of the obesity‐colorectal neoplasia link. The homeostasis model assessment‐IR (HOMA‐IR) is a widely accepted index of evolving hyperinsulinemia and early IR. Studies of the relation between HOMA‐IR and colorectal adenomas are limited. Therefore, the authors sought to determine the associations of HOMA‐IR and central obesity (waist to hip ratio [WHR]) with risk of colorectal adenomas in a screening colonoscopy‐based study.

METHODS:

The authors collected lifestyle information and fasting blood samples from 1222 participants (320 incident adenoma cases and 902 without adenomas) before their screening colonoscopies. Unconditional logistic regression models were used to assess risk associations.

RESULTS:

In multivariate analysis of participants (n = 1093) reporting no antidiabetic medication use, those in the top quartile of WHR were twice as likely (odds ratio [OR], 2.18; 95% confidence interval [CI], 1.33‐3.57; P‐trend = .003) and those in the top quartile of HOMA‐IR were 63% more likely (OR, 1.63; 95% CI, 1.09‐2.44; P‐trend = .01) to have adenomas compared with those in the bottom quartiles. Stratified analysis revealed a statistically significant interaction between HOMA‐IR and sex (P‐interaction = .04), with the association largely limited to men; compared with those in the bottom tertile, men in the top tertile of HOMA‐IR were twice more likely to have adenomas (OR, 2.11; 95% CI, 1.18‐3.78; P‐trend = .01).

CONCLUSIONS:

The results support central obesity and insulin resistance, particularly in men, as important risk factors for the development of early colorectal neoplasia. Cancer 2012;. © 2011 American Cancer Society.
Ultrashort courses of adjuvant breast radiotherapy
Authors: Khan Atif J. , Dale Roger G. , Arthur Douglas W. , Haffty Bruce G. , Todor Dorin A. , Vicini Frank A.
Published: September 2011

In accelerated partial breast irradiation (APBI), the most commonly used fractionation schemes include 340 or 385 centigrays delivered in a twice daily administration. A further progression of the APBI literature has been the recent interest in extremely short courses of adjuvant radiotherapy, usually delivered by intraoperative radiotherapy techniques. This newer area of single‐fraction radiotherapy approaches remains highly contentious. In particular, the recently reported TARGIT trial has been the subject of both praise and scorn, and a critical examination of the trial data and the underlying hypotheses is warranted. Short‐term outcomes of the related Italian ELIOT approach have also been reported. Although the assumptions of linear quadratic formalism are likely to hold true in the range of 2 to 8 grays, equating different schedules beyond this range is problematic. A major problem of current single‐fraction approaches is that the treatment doses are chosen empirically, or are based on tolerability, or on the physical dose delivery characteristics of the chosen technology rather than radiobiological rationale. This review article summarizes the current data on ultrashort courses of adjuvant breast radiotherapy and highlights both the promise and the potential pitfalls of the abbreviated treatment. Cancer 2012. © 2011 American Cancer Society.
Occult axillary lymph node metastases do not have prognostic significance in early stage breast cancer
Authors: Wu Yun , Mittendorf Elizabeth A. , Kelten Canan , Tucker Susan L. , Wei Wei , Middleton Lavinia P. , Broglio Kristine , Buchholz Thomas A. , Hunt Kelly K. , Sahin Aysegul A.
Published: September 2011

BACKGROUND:

Axillary lymph node status is one of the most powerful prognostic indicators in patients with breast cancer and has implications for adjuvant treatment. It has been demonstrated that enhanced histologic evaluation of axillary lymph nodes, including serial sectioning of paraffin tissue blocks and immunohistochemical (IHC) staining, increases the rate of detection of occult metastases. The clinical significance of occult lymph node metastases has been the subject of debate.

METHODS:

In the current study, the authors identified 267 patients who underwent axillary lymph node dissection (ALND) between 1987 and 1995 and were lymph node negative according to a routine pathologic evaluation, which included the complete submission of all lymph nodes and an examination of 1 hematoxylin and eosin (H&E)‐stained section per paraffin block. Patients did not receive systemic chemotherapy or hormone therapy. All of the dissected lymph nodes from these patients were re‐evaluated by intensified pathologic methods (serial sectioning with H&E levels plus IHC). Occult metastases were categorized by detection method and size. The clinical significance of the occult metastases was determined.

RESULTS:

Thirty‐nine patients (15%) who had lymph node‐negative results on routine evaluation of their ALND specimens had occult metastases identified. Eight of these patients (20%) had macrometastases >2.0 mm, 15 (40%) had micrometastases (range, >0.2 mm to ≤2 mm), and 16 (40%) had isolated tumor cells (≤0.2 mm). The presence of occult metastases and the size of metastases did not affect recurrence‐free or overall survival.

CONCLUSIONS:

The presence of occult metastasis did not have clinical significance in this cohort of patients with early stage breast cancer. Cancer 2011;. © 2011 American Cancer Society.
Noninvasive and real‐time monitoring of the therapeutic response of tumors in vivo with an optimized hTERT promoter
Authors: Yu Song‐Tao , Li Chuan , Lü Mu‐Han , Liang Guang‐Ping , Li Ning , Tang Xu‐Dong , Wu Yu‐Yun , Shi Chun‐Meng , Chen Ling , Li Chang‐Zhu , Cao Ya‐Ling , Fang Dian‐Chun , Yang Shi‐Ming
Published: September 2011

BACKGROUND:

Telomerase is commonly recognized as an effective anticancer target. The human telomerase reverse transcriptase (hTERT), the rate‐limiting component of telomerase, is expressed in most malignant tumors, but it is not found in most normal somatic cells. Here, we report a real‐time and noninvasive method to monitor tumor response to a lentivirus‐based hTERT‐conditional suicidal gene therapy.

METHODS:

In this study, we constructed a lentivirus system in which an optimized hTERT promoter was used to drive the expression of the cytosine deaminase (CD) gene, one of the suicide genes, and a green fluorescent protein (GFP) reporter gene (pLenti‐CD/GFP). The lentivirus was used to infect telomerase‐positive or telomerase‐negative cell lines. In vitro and in vivo experiments were conducted to analyze the dynamic processes of exogenous gene expression noninvasively in cell culture and living animals in real time via optical imaging.

RESULTS:

The lentivirus was able to express the CD gene and GFP in telomerase‐positive tumor cells and significantly decrease cell proliferation after the use of prodrug 5‐flucytosine. However, it could not express GFP and CD in telomerase‐negative cell lines, nor could it induce any suicidal effect in those cells. The in vivo study showed that telomerase‐positive tumors can be visualized after intratumor injection of the lentivirus in tumor‐bearing nude mice via an optical imaging system. Significant tumor growth suppression was observed in telomerase‐positive tumors.

CONCLUSIONS:

Collectively, this technology provides a valuable, noninvasive method to evaluate the real‐time therapeutic response of tumors in vivo. Cancer 2012;. © 2011 American Cancer Society.
Impact of androgen deprivation therapy on depressive symptoms in men with nonmetastatic prostate cancer
Authors: Timilshina Narhari , Breunis Henriette , Alibhai Shabbir
Published: September 2011

BACKGROUND:

Up to 50% of prostate cancer (PC) patients receive androgen deprivation therapy (ADT), often for several years. Although depression has been reported after a diagnosis of PC, whether ADT leads to or worsens depression is not clear.

METHODS:

Three groups were assembled: ADT users (men initiating continuous ADT), PC controls (PC patients who were not on ADT), and healthy controls. All 3 cohorts were matched on age, education, and physical function, and none had metastases. Depression was measured at study entry and again at 3, 6, and 12 months using the 15‐item Geriatric Depression Scale (GDS). Our primary outcomes were worsening depressive symptoms and incident depression (defined as a GDS score ≥5), analyzed using adjusted linear regression and logistic regression, respectively.

RESULTS:

Of the 257 participants (mean age, 69.1 years), baseline characteristics including GDS score and prior depression were similar across cohorts. In adjusted analyses of initially nondepressed patients, ADT use was not a significant predictor of change in GDS score at 3 months (P = .42), 6 months (P = .25), or 12 months (P = 0.19). Among ADT users, 8%‐9% of participants developed incident depression compared with 0%‐4% among PC controls and 4%‐6% among healthy controls over 3‐12 months (P>.05 at all time points). In a separate analysis of patients with depression at baseline, there was no effect of ADT on depressive symptoms at 3, 6, or 12 months (P = .11, .74, and .12, respectively).

CONCLUSION:

Twelve months of ADT use were not associated with worsening depressive symptoms among nondepressed or depressed patients with nonmetastatic PC. Cancer 2012;. © 2011 American Cancer Society.
Disparities in cancer screening in individuals with a family history of breast or colorectal cancer
Authors: Ponce Ninez A. , Tsui Jennifer , Knight Sara J. , Afable‐Munsuz Aimee , Ladabaum Uri , Hiatt Robert A. , Haas Jennifer S.
Published: September 2011

BACKGROUND:

Understanding racial/ethnic disparities in cancer screening by family history risk could identify critical opportunities for patient and provider interventions tailored to specific racial/ethnic groups. The authors evaluated whether breast cancer (BC) and colorectal cancer (CRC) disparities varied by family history risk using a large, multiethnic population‐based survey.

METHODS:

By using the 2005 California Health Interview Survey, BC and CRC screening were evaluated separately with weighted multivariate regression analyses, and stratified by family history risk. Screening was defined for BC as mammogram within the past 2 years for women aged 40 to 64 years; for CRC, screening was defined as annual fecal occult blood test, sigmoidoscopy within the past 5 years, or colonoscopy within the past 10 years for adults aged 50 to 64 years.

RESULTS:

The authors found no significant BC screening disparities by race/ethnicity or income in the family history risk groups. Racial/ethnic disparities were more evident in CRC screening, and the Latino‐white gap widened among individuals with family history risk. Among adults with a family history for CRC, the magnitude of the Latino‐white difference in CRC screening (odds ratio [OR], 0.28; 95% confidence interval [CI], 0.11‐0.60) was more substantial than that for individuals with no family history (OR, 0.74; 95% CI, 0.59‐0.92).

CONCLUSIONS:

Knowledge of their family history widened the Latino‐white gap in CRC screening among adults. More aggressive interventions that enhance the communication between Latinos and their physicians about family history and cancer risk could reduce the substantial Latino‐white screening disparity in Latinos most susceptible to CRC. Cancer 2011;. © 2011 American Cancer Society.
Heat shock factor 1 promotes invasion and metastasis of hepatocellular carcinoma in vitro and in vivo
Authors: Fang Feng , Chang Ruimin , Yang Lianyue
Published: September 2011

BACKGROUND:

Heat shock factor 1 (HSF1) is a powerful, multifaceted modifier of carcinogenesis. However, the clinical significance and biologic function of HSF1 in hepatocellular carcinoma (HCC) remain unknown.

METHODS:

Quantitative reverse transcriptase‐polymerase chain reaction analysis, Western blot analysis, and immunohistochemical staining were used to detect expression levels of HSF1, and its correlation with clinicopathologic parameters and the prognosis for patients with HCC were analyzed. In addition, the biologic function and molecular mechanisms of HSF1 in HCC were investigated in vitro and in vivo.

RESULTS:

HSF1 levels were elevated predominantly in HCC, especially in venous emboli from HCC (P < .05), and high expression levels of HSF1 were correlated significantly with multiple nodules, venous invasion, absence of capsular formation, and high Edmondson‐Steiner grade as well as poor overall survival and disease‐free survival in patients with HCC (P < .05). Multivariate Cox regression analysis revealed that high HSF1 expression was an independent prognostic factor for overall survival in patients with HCC (relative risk, 4.874; P < .001). Finally, HSF1 was capable of promoting HCC cell migration and invasion in vitro and in vivo by facilitating the expression and phosphorylation of heat shock protein 27.

CONCLUSIONS:

Collectively, the current findings suggested that HSF1 may serve as a novel prognostic marker and therapeutic target for HCC. Cancer 2012;. © 2011 American Cancer Society.
Interval to biochemical failure as a biomarker for cause‐specific and overall survival after dose‐escalated external beam radiation therapy for prostate cancer
Authors: Kapadia Nirav S. , Olson Karin , Sandler Howard M. , Feng Felix Y. , Hamstra Daniel A.
Published: September 2011

BACKGROUND:

After external beam radiation therapy (EBRT) for prostate cancer, a short interval to biochemical failure of <18 months has been proposed as a surrogate for cause‐specific survival. Because EBRT dose influences biochemical failure, the authors investigated the interval to biochemical failure in a cohort of patients treated with dose‐escalated EBRT.

METHODS:

From 1998 to 2008, 710 patients were treated with EBRT (≥75 grays) ± androgen deprivation therapy (ADT) at the University of Michigan. Biochemical failure was defined using the Phoenix consensus definition (nadir + 2 ng/mL). A short interval to biochemical failure was defined as <18 months after completing radiotherapy and/or ADT. The associations between biochemical failure, the interval to biochemical failure, and clinical factors with cause‐specific survival (CSS) and overall survival (OS) were evaluated.

RESULTS:

There were 149 biochemical failures (21%), and short interval to biochemical failure accounted for 14% and 40% of biochemical failures in those with intermediate‐risk or high‐risk disease, respectively. Biochemical failure impacted CSS (P < .0001) but not OS (P = .36). However, a short interval to biochemical failure predicted decreased CSS (P < .0001; hazard ratio [HR], 5.6; 95% confidence interval [CI], 2.4‐13.0) and OS (P < .0001; HR, 4.8; 95% CI, 2.3‐10.3) when compared with a long interval to biochemical failure. The 8‐year OS was 78% without biochemical failure, compared with 87% with a long interval to biochemical failure (P = .1; HR, 0.7; 95% CI, 0.4‐1.1) and 38% with a short interval to biochemical failure (P < .0001; HR, 3.7; 95% CI, 2.3‐5.9). On multivariate analysis, a short interval to biochemical failure increased the risk of prostate cancer death (P < .0001; HR, 18.1; 95% CI, 8.4‐39) and all cause mortality (P = .0027; HR, 1.5; 95% CI, 1.2‐2.1), whereas a long interval to biochemical failure did not.

CONCLUSIONS:

The relation between the interval to biochemical failure, CSS, and OS was independently validated in patients treated with dose‐escalated EBRT. Further evaluation of the interval to biochemical failure as a surrogate endpoint is warranted. Cancer 2012. © 2011 American Cancer Society.