bluuebunny/crossref_metadata_2025 huggingface dataset:
ChemInform Abstract: Copper(II)‐Catalyzed Esterification of Arenecarboxylic Acids with Aryl‐ and Vinyl‐Substituted Trimethoxysilanes.
Authors: Luo Fang , Pan Changduo , Qian Pengcheng , Cheng Jiang
Published: September 2010

The method represents a practical alternative without the need of acyl chlorides and phenols as substrates.
ChemInform Abstract: Selenium‐Catalyzed Oxidative Carbonylation of Aniline and Alcohols to N‐Phenylcarbamates.
Authors: Zhang Xiaopeng , Jing Huanzhi , Zhang Guisheng
Published: September 2010

A facile one‐pot, phosgene‐free synthesis of N‐phenylcarbamates (IV) is demonstrated.
ChemInform Abstract: Cationic Pd(II)/Bipyridine‐Catalyzed Conjugate Addition of Arylboronic Acids to β,β‐Disubstituted Enones: Construction of Quaternary Carbon Centers.
Authors: Lin Shaohui , Lu Xiyan
Published: September 2010

Low amounts of the complex PBB allow the preparation of various β‐disubstituted cyclohexanone derivatives and cyclopentanone (IIIb) in good to excellent yield.
ChemInform Abstract: i‐PrI Acceleration of Negishi Cross‐Coupling Reactions.
Authors: Kienle Marcel , Knochel Paul
Published: September 2010

The reaction of bisorganyl zinc reagents with bromoanilines, bromoketones and various aryl bromides, bearing acidic benzylic protons lead to the corresponding bisaryls in high yields.
ChemInform Abstract: Development of Binaphthyl‐Based Chiral Dienes for Rhodium(I)‐Catalyzed Asymmetric Arylation of N,N‐Dimethylsulfamoyl‐Protected Aldimines.
Authors: Cao Ziping , Du Haifeng
Published: September 2010

Ten ligands bearing aromatic substituents are prepared and the anisyl derivative (I) is found to be the most efficient one.
ChemInform Abstract: A Convenient Synthesis of (Z)‐4‐Hydroxy‐N‐desmethyltamoxifen (Endoxifen).
Authors: Fauq Abdul H. , Maharvi Ghulam M. , Sinha Dola
Published: September 2010

A convenient synthesis of (Z)‐4‐hydroxy‐N‐desmethyltamoxifen (endoxifen) (IV), a potent antiestrogenic metabolite of the anticancer drug tamoxifen, is presented.
ChemInform Abstract: Fast Copper‐, Ligand‐ and Solvent‐Free Sonogashira Coupling in a Ball Mill.
Authors: Thorwirth Rico , Stolle Achim , Ondruschka Bernd
Published: September 2010

Palladium acetate as catalyst in combination with SiO2 as a grinding auxiliary allow for the chemoselective transformation of aryl iodides.
ChemInform Abstract: Palladium‐Catalyzed Direct Cross‐Coupling Reaction Between Indenes and Electron‐Deficient Alkenes.
Authors: Xu Yun‐He , Wang Wee‐Jian , Wen Zhen‐Kang , Hartley Joshua Jonathan , Loh Teck‐Peng
Published: September 2010

The simple procedure affords the desired dienes in moderate to low yields.
ChemInform Abstract: An Open‐and‐Shut Strategy: Preparation of Benzofused Indans by Ring‐Opening of a Vinylogous Acyl Triflate and Metal‐Catalyzed Asao—Yamamoto Benzannulation.
Authors: Jones David M. , Dudley Gregory B.
Published: September 2010

A combination of tandem addition—fragmentation of vinylogous acyl triflates (II), (XII) towards iodobenzene derivatives and intramolecular benzannulation of o‐alkynylphenyl ketones (VI) and (XIII) is successfully applied as novel strategy for the synthesis of benzofused indans.
ChemInform Abstract: Synthesis of Bishomobenzoctamine 2‐(9,10‐Dihydro‐9,10‐propanoanthracen‐9‐yl)‐N‐methylethanamine (IX)
Authors: Karama Usama , Al‐Saidey Adel , Almansour Abdel Rahman
Published: September 2010

[via an ultrasound‐assisted [3 + 4] cycloaddition of allylanthracene (III) with tetrabromoacetone].
ChemInform Abstract: Cyclopentadienylcobalt‐Mediated Intermolecular Cycloaddition of α,ω‐Diynes to (Cyclo)alkenes: Synthesis of Linearly Fused Oligocycles and Extension to Enantiomerically Pure (6aR,10aR)‐Dihydroanthracyclinones.
Authors: Aubert Corinne , Gandon Vincent , Han Sangdon , Johnson Barry M. , Malacria Max , Schoemenauer Sten , Vollhardt K. Peter C. , Whitener Glenn D.
Published: September 2010

The [2 + 2 + 2] photocycloaddition of diynes with a broad spectrum of nonactivated 1,2‐disubstituted alkenes is investigated in the presence of CpCo(CO)2.
ChemInform Abstract: Asymmetric Epoxidation of 2‐Arylidene‐1,3‐diketones: Facile Access to Synthetically Useful Epoxides.
Authors: Russo Alessio , Lattanzi Alessandra
Published: September 2010

The first asymmetric epoxidation of title arylidenediketones, e.g. (I), (IV) or (VI), is presented.
ChemInform Abstract: Isothiourea‐Mediated Stereoselective C‐Acylation of Silyl Ketene Acetals.
Authors: Woods Philip A. , Morrill Louis C. , Lebl Tomas , Slawin Alexandra M. Z. , Bragg Ryan A. , Smith Andrew D.
Published: September 2010

The optimized conditions are applied to the preparation of 22 derivatives.
ChemInform Abstract: Application of Dicyclohexyl‐(S)‐trimethoxyphenyl Phosphine·HBF4 Salt for the Highly Selective Suzuki Coupling of the C—Cl Bond in β‐Chlorobutenolides Over the More Reactive Allylic C—O Bond.
Authors: Lue Bo , Fu Chunling , Ma Shengming
Published: September 2010

A newly developed ligand is used for the selective Suzuki coupling of β‐chlorobutenolides with arylboronic acids giving products with high enantioselectivities.
ChemInform Abstract: PEG 400 as a Reusable Solvent for 1,4‐Dipolar Cycloadditions via a Three‐Component Reaction.
Authors: Reddy B. V. Subba , Somashekar D. , Reddy A. Mallikarjun , Yadav J. S. , Sridhar Balasubramanian
Published: September 2010

Polyethylene glycol 400 represents an efficient reaction medium for the cycloaddition of α,β‐unsaturated aromatic aldehydes with zwitterions derived from isocyanides and dialkyl acetylenedicarboxylates to give styryl‐ and chromenylfurans in good yields.
ChemInform Abstract: A Synthesis of β‐Allyl Substituted Isotetronic Acid Derivatives via Thermal Claisen Rearrangement.
Authors: Ma Xiaping , Li Zhiming , Wang Quanrui
Published: September 2010

The Claisen rearrangement of O‐allyl substituted isotetronic acids of type (I), (III), or (V) is described.
ChemInform Abstract: Asymmetric Synthesis of Thiadecalins via an Organocatalytic Triple Cascade/ Sulfa‐Michael Sequence.
Authors: Enders Dieter , Schmid Bertram , Erdmann Nico , Raabe Gerhard
Published: September 2010

A two‐step route consisting of a triple domino reaction of aldehydes (I) or (VI), β‐nitrostyrenes and α,β‐unsaturated aldehydes (III) or (IX) followed by an intermolecular sulfa‐Michael addition offers a convenient synthesis to the thiadecalin skeleton and a related benzothiophene (VIII).
ChemInform Abstract: Synthesis and Antimicrobial Evaluation of Some New Thiophene Derivatives.
Authors: Khalil A. M. , Berghot M. A. , El‐Ghani Ghada E. Abd , Gouda M. A.
Published: September 2010

Representative compounds are evaluated for their antibacterial (Bacillus thuringiensis, Klebsiella pneumoniae) and antifungal (Botrytis fabae, Fusarium oxysporum) activities.
ChemInform Abstract: Novel 1,3,5‐Triphenyl‐2‐pyrazolines as Antiinfective Agents.
Authors: Sivakumar P. M. , Seenivasan S. Prabhu , Kumar Vanaja , Doble Mukesh
Published: September 2010

A series of 16 compounds of type (III) or (IV) are tested as anti‐infective agents.
ChemInform Abstract: Synthesis of 4‐Aryl‐1H‐pyrazoles by Suzuki—Miyaura Cross Coupling Reaction Between 4‐Bromo‐1H‐1‐tritylpyrazole and Arylboronic Acids.
Authors: Ichikawa Hayato , Nishioka Miho , Arimoto Masao , Usami Yoshihide
Published: September 2010

A general method is presented for the preparation of title compounds (III).
ChemInform Abstract: Potassium Dihydrogen Phosphate Catalyzed One‐Pot Synthesis of 2,4,5‐Triaryl‐1H‐imidazoles.
Authors: Joshi Ratnadeep S. , Mandhane Priyanka G. , Shaikh Mohammad U. , Kale Rajesh P. , Gill Charansingh H.
Published: September 2010

Compared to benzoin (III), benzil (I) affords marginally higher yields in shorter reaction times.
ChemInform Abstract: Synthesis of 2,4,5‐Triarylimidazoles in Aqueous Solution, under Microwave Irradiation.
Authors: Chauveau Edouard , Marestin Catherine , Schiets Frederic , Mercier Regis
Published: September 2010

The three‐component reaction presented proceeds expeditiously and with excellent yields, affording the title compounds (III) by simple filtration.
ChemInform Abstract: Versatile Synthesis of Quaternary 1,3‐Oxazolidine‐2,4‐diones and Their Use in the Preparation of α‐Hydroxyamides.
Authors: Merino Omar , Santoyo Blanca M. , Montiel Luisa E. , Jimenez‐Vazquez Hugo A. , Zepeda L. Gerardo , Tamariz Joaquin
Published: September 2010

A new two‐step sequence involves reaction of α‐ketols with isocyanates and subsequent oxidative cleavage of the exocyclic double bond according to A) or B) to give the title compounds.
ChemInform Abstract: Gold‐Catalyzed Cyclization and Subsequent Arylidene Group Transfer of O‐Propioloyl Oximes.
Authors: Nakamura Itaru , Okamoto Masashi , Terada Masahiro
Published: September 2010

The simple procedure allows the cycloisomerization of (E)‐oximes derived from aromatic aldehydes (or ketones) to 4‐arylideneisoxazolones with high (Z)‐selectivity.The substrate (V) bearing an alkyl group does not react but decomposes spontaneously.
ChemInform Abstract: Direct Synthesis of Trisubstituted Isoxazoles Through Gold‐Catalyzed Domino Reaction of Alkynyl Oxime Ethers.
Authors: Ueda Masafumi , Sato Aoi , Ikeda Yuki , Miyoshi Tetsuya , Naito Takeaki , Miyata Okiko
Published: September 2010

The novel method allows the approach to various trisubstituted isoxazoles, which may be of interest in natural product synthesis and as biological substances.
ChemInform Abstract: An Efficient Synthesis of Highly Functionalized 4H‐Pyrano[3,2‐d]isoxazoles via Isocyanide‐Based Three‐Component Reaction.
Authors: Esmaeili Abbas Ali , Hosseinabadi Rahele , Habibi Azizollah
Published: September 2010

Zwitterionic intermediates generated from isocyanides and diesters (II) react with isoxazolone (I) to produce the title compounds (IV) in good yields.
ChemInform Abstract: A Highly Efficient Methodology for 5‐Methyl‐3‐aryl‐2‐thiooxazolidin‐4‐ones Using Lithium Perchlorate in DIPEA Mediated Synthesis.
Authors: Khatik Gopal L. , Pal Anang , Apsunde Tushar D. , Nair Vipin A.
Published: September 2010

Aryl isothiocyanates (III) are converted to the title compounds (V) by treating with ethyl lactate (IV) in the presence of a base and a catalytic amount of lithium perchlorate.
ChemInform Abstract: Copper(I)‐Catalyzed Azide—Alkyne Cycloadditions in Ionic Liquids under Amine‐Free Conditions.
Authors: Vecchi Alessandra , Chambery Angela , Chiappe Cinzia , Marra Alberto , Dondoni Alessandro
Published: September 2010

The commercially available polyoxygenated ionic liquid AMMOENG 100 promotes the reaction of structurally diverse azides with different terminal alkynes without the need for amines as an additive.
ChemInform Abstract: Copper Nitride Nanoparticles Supported on a Superparamagnetic Mesoporous Microsphere for Toxic‐Free Click Chemistry.
Authors: Chi Dae Yoon , et al. et al.
Published: September 2010

Copper nitride nanoparticles supported on a mesoporous superparamagnetic silica microsphere exhibit superior catalytic activity toward the Huisgen cycloaddition of azides and alkynes (15 examples).
ChemInform Abstract: Novel and Practical Synthesis of Candesartan Cilexetil.
Authors: Mao Yongjun , Xiong Ruisheng , Liu Zheng , Li Haihong , Shen Jingkang , Shen Jingshan
Published: September 2010

A novel synthesis of candesartan cilexetil (VII) is described.
ChemInform Abstract: Lewis Acid Catalyzed Cycloaddition of Methylenecyclopropanes with Salicylaldehydes.
Authors: Jiang Min , Shi Min
Published: September 2010

Treatment of salicylaldehydes with triethyl orthoformate generates o‐quinonemethide analogues which undergo efficient Lewis acid catalyzed cycloaddition with methylenecyclopropanes to produce the desired benzopyran products.
ChemInform Abstract: Synthesis of Chromeno[3,4‐b]pyrrol‐4(3H)‐ones by Cyclocondensation of 1,3‐Bis(trimethylsilyloxy)buta‐1,3‐dienes with 4‐Chloro‐3‐nitrocoumarin.
Authors: Fatunsin Olumide , Iaroshenko Viktor O. , Dudkin Sergii , Shkoor Mohanad , Volochnyuk Dmitro , Gevorgyan Ashot , Langer Peter
Published: September 2010

The highly efficient two‐step sequence is suitable for application in medicinal chemistry.
ChemInform Abstract: The Discovery and Structure—Activity Relationships of 2‐(Piperidin‐3‐yl)‐1H‐Benzimidazoles as Selective, CNS Penetrating H1‐Antihistamines for Insomnia.
Authors: Beaton Graham , et al. et al.
Published: September 2010

A series of novel benzimidazoles (VII) are synthesized and identified as potent and selective H1‐antihistamines with reduced hERG activity.
ChemInform Abstract: Selective and Facile Palladium‐Catalyzed Amination of 2‐Fluoro‐4‐iodopyridine in the 4‐Position under Microwave Conditions.
Authors: Koley Moumita , Schnuerch Michael , Mihovilovic Marko D.
Published: September 2010

The microwave protocol is superior to previous procedures due to drastically shorter reaction times and significantly decreased amounts of base.
ChemInform Abstract: Facile Synthesis and Antibacterial, Antitubercular, and Anticancer Activities of Novel 1,4‐Dihydropyridines.
Authors: Sirisha Kalam , Achaiah Garlapati , Reddy Vanga Malla
Published: September 2010

Improved Hantzsch syntheses under different conditions are applied for the preparation of a series of heteroaryl substituted DHP′s.
ChemInform Abstract: A New Synthesis of (R)‐(‐)‐Sumanirole (PNU‐95666E).
Authors: Jean‐Gerard Ludivine , Mace Frederic , Dentel Helene , Ngo Anh Ngoc , Collet Sylvain , Guingant Andre , Evain Michel
Published: September 2010

The title compound (VI) was investigated in clinical studies for the treatment of Parkinson′s disease and found to be unsuitable.
ChemInform Abstract: Synthesis of 7‐Benzyl‐5‐(piperidin‐1‐yl)‐6,7,8,9‐tetrahydro‐3H‐pyrazolo[3,4‐c] [2,7]naphthyridin‐1‐ylamine and Its Analogues as Bombesin Receptor Subtype‐3 Agonists.
Authors: Guo Cheng , et al. et al.
Published: September 2010

A concise synthesis of the title compound (VI) in gram quantity is achieved starting from commercially available materials.
ChemInform Abstract: The Synthesis of 3‐Pyrazinyl‐imidazo[1,2‐a]pyridines from a Vinyl Ether.
Authors: Collins Michael Raymond , Huang Qinhua , Ornelas Martha A. , Scales Stephanie A.
Published: September 2010

Treatment of vinyl ether (II) with NBS and water generates the brominated hemiacetal intermediate (III) which reacts with aminopyridines to afford the pharmaceutically important skeleton (IV) in moderate yields.
ChemInform Abstract: Concise Copper‐Catalyzed One‐Pot Tandem Synthesis of Benzimidazo[1,2‐b]isoquinolin‐11‐one Derivatives.
Authors: Lu Juyou , Gong Xiaoyu , Yang Haijun , Fu Hua
Published: September 2010

Title compounds (III) are formed via coupling of 2‐halo‐N‐(2‐halophenyl)benzamides (I) with 2‐cyanoacetates or malononitrile (II).
ChemInform Abstract: Synthesis of Thiopyrano[4′′,3′′:4′,5′]pyrido[3′,2′:4,5]furo[3,2‐d]pyrimidines.
Authors: Ahmed Essam Kh. , Ameen Mohamed A.
Published: September 2010

Starting from substrates (I), the title skeleton (VI) is prepared via tricyclic precursors of type (II).
ChemInform Abstract: Efficient Formation of 4,6‐Disubstituted Pyrrolo[2,3‐d]pyrimidines: A Novel Route to TWS119, a Glycogen Synthase Kinase‐3β Inhibitor.
Authors: Mayasundari Anand , Fujii Naoki
Published: September 2010

A convenient method is developed which proceeds via base‐promoted microwave cyclization of alkynes of type (I).
ChemInform Abstract: 4‐Hydroxy‐2‐quinolones. Part 173. 1‐R‐3‐(2‐Diethylaminoethyl)‐1H‐quinazoline‐2,4‐dione Hydrochlorides as Potential Local Anesthetic Agents.
Authors: Ukrainets I. V. , Kravtsova V. V. , Tkach A. A. , Mamchur V. I. , Kovalenko E. Yu.
Published: September 2010

A variety of new title aminoethylquinazolinedione derivatives having structural similarities to the 4‐hydroxy‐2‐quinolinone anesthetic chinoxicaine are synthesized and evaluated for their anesthesia penetration, motor block and sedative effect compared to chinoxicaine and lidocaine.
ChemInform Abstract: A Simple and Efficient Synthesis of the Antimigraine Drug Lomerizine (IV).
Authors: Narsaiah A. Venkat , Kumar J. Kranthi
Published: September 2010

The process is amenable to large‐scale synthesis.
ChemInform Abstract: Silica Gel‐Promoted Tandem Addition—Cyclization Reactions of 2‐Alkynylbenzenamines with Isothiocyanates.
Authors: Ding Qiuping , Cao Banpeng , Zong Zhenzhen , Peng Yiyuan
Published: September 2010

The title reaction offers the advantages of easy work‐up, metal‐ and solvent‐free conditions, and a recoverable (four cycles with ca. 10% loss of activity) and readily available catalyst.
ChemInform Abstract: An Unprecedented and Concise Method for the Synthesis of 1,3‐Thiazino‐[3,4‐a][1,3]benzimidazoles via a Three‐Component Reaction.
Authors: Alizadeh Abdolali , Noaparast Zohreh , Sabahnoo Hamideh , Zohreh Nasrin
Published: September 2010

The novel and simple protocol allows the synthesis of the biologically interesting title compounds (IV).
ChemInform Abstract: Enantioconservative Synthesis of Polysubstituted Pyrimido[4,5‐b]azepines.
Authors: Gerig Britta , Girreser Ulrich , Schuett Martin , Heber Dieter
Published: September 2010

The three‐step synthesis of the title compounds, which have a high potential as adenosine receptors, is based on a Dieckmann cyclization of racemic cyano esters (V) and chiral cyano ester (IX).
ChemInform Abstract: Mild Silver(I)‐Mediated Regioselective Iodination and Bromination of Arylboronic Acids.
Authors: Al‐Zoubi Raed M. , Hall Dennis G.
Published: September 2010

Direct ortho‐halogenation is possible for a broad spectrum of substrates under the optimized conditions.
ChemInform Abstract: HClO4—SiO2 as a Novel and Recyclable Catalyst for the Phospha‐Michael Addition of Phosphorous Nucleophiles to α,β‐Unsaturated Malonates.
Authors: Sobhani Sara , Rezazadeh Soodabeh
Published: September 2010

The desired products are obtained within a short time.
ChemInform Abstract: Preparation of Functionalized Cyclic Enol Phosphates by Halogen—Magnesium Exchange and Directed Deprotonation Reactions.
Authors: Piller Fabian M. , Bresser Tomke , Fischer Markus K. R. , Knochel Paul
Published: September 2010

A wide range of functionalized cyclic enol phosphates can be prepared.
ChemInform Abstract: Palladium‐Catalyzed Alkynylselenation of Acetylenedicarboxylates Leading to Enyne Selenides and Application to Synthesis of Multisubstituted Aryl Selenides.
Authors: Mitamura Takenori , Ogawa Akiya
Published: September 2010

The type of catalyst controls the course of the reactions to give either (E)/(Z)‐mixtures (III)/(IV) or the aryl selenides (V) and (VII).
ChemInform Abstract: Novel Axially Chiral Phosphine Ligand with a Fluoro Alcohol Moiety for Rh‐Catalyzed Asymmetric Arylation of Aromatic Aldehydes.
Authors: Morikawa Satoshi , Michigami Kyosuke , Amii Hideki
Published: September 2010

BNF is found to be highly effective for the addition of arylboronic acids to aromatic aldehydes and is thus of interest in the preparation of bioactive diaryl methanols.
ChemInform Abstract: Oppositane‐Type Sesquiterpenoids from the Formosan Soft Coral Sinularia leptoclados
Authors: Huang Chiung‐Yao , Su Jui‐Hsin , Liu Yung‐Chun , Wen Zhi‐Hong , Hsu Chi‐Hsin , Chiang Michael Y. , Sheu Jyh‐Horng
Published: September 2010

structure determination and cytotoxicity of the new sesquiterpenoids leptocladolin A (I) and B (II) and two known compounds
ChemInform Abstract: Glandular Trichomes of Leucosceptrum canum Harbor Defensive Sesterterpenoids.
Authors: Luo Shi‐Hong , Luo Qian , Niu Xue‐Mei , Xie Ming‐Jin , Zhao Xu , Schneider Bernd , Gershenzon Jonathan , Li Sheng‐Hong
Published: September 2010

Leucosceptroid A (I) and leucosceptroid B (II) are found to be the major metabolites of the trichomes of L.
ChemInform Abstract: Novel anti‐β‐Functionalized γ,δ‐Unsaturated Amino Acids via a Thio‐Claisen Rearrangement.
Authors: Liu Zhihua , Qu Hongchang , Gu Xuyuan , Lee Kwang‐Soo , Grossman Bryan , Kumirov Vlad K. , Hruby Victor J.
Published: September 2010

A significantly improved approach to novel title compounds is developed.
ChemInform Abstract: Synthesis and Antitumor Activities of Methyl 2‐O‐Aryl‐6‐O‐aryl′‐D‐glucopyranosides.
Authors: Shi Hefang , Zhou Bingcheng , Li Wenwen , Shi Zhimin , Yu Biao , Wang Renxiao
Published: September 2010

A new synthetic method to introduce bulky aryl groups at both the 2‐O‐ and 6‐O‐position on D‐glucopyranoside is developed.
ChemInform Abstract: Direct α‐Selective Glycosylations of Acetyl‐Protected 2‐Deoxy‐ and 2,6‐Dideoxythioglycosides by Preactivation Protocol.
Authors: Lu Yin‐Suo , Li Qin , Wang Yuan , Ye Xin‐Shan
Published: September 2010

Thioglycoside donors (II), (V) and (IX) are preactivated according to A).
ChemInform Abstract: Approaches to N‐Methylwelwitindolinone C Isothiocyanate (XI): Facile Synthesis of the Tetracyclic Core.
Authors: Heidebrecht Richard W. Jr. , Gulledge Brian , Martin Stephen F.
Published: September 2010

A straightforward entry to the tetracyclic compound (X), which represents the core structure found in the title compound, is developed.
ChemInform Abstract: Synthesis of (+)‐Lycoricidine by the Application of Oxidative and Regioselective Ring‐Opening of Aziridines.
Authors: Vadav J. S. , Satheesh G. , Murthy Changalvala V. S. R.
Published: September 2010

A simple two‐step procedure which involves oxdiation of alcohols, derived from (D)‐(+)‐mannose, and silica gel mediated regioselective ring opening of the resulting ketones provides amines such as (II) and (V).
ChemInform Abstract: Total Synthesis of (+)‐Stachyflin: A Potential Antiinfluenza A Virus Agent.
Authors: Watanabe Kazuhiro , Sakurai Junji , Abe Hideki , Katoh Tadashi
Published: September 2010

The first enantioselective total synthesis of (+)‐stachyflin (VI) is reported.
ChemInform Abstract: Synthesis of the Bis‐spiroacetal C25—C40 Moiety of the Antimitotic Agent Spirastrellolide B Using a Bis‐dithiane Deprotection/Spiroacetalisation Sequence.
Authors: Chen Jack Li‐Yang , Brimble Margaret A.
Published: September 2010

The [5,6,6]‐bis‐spiroacetal moiety (II) of spirastrellolide B is prepared via a HgCl2‐mediated double dithiane deprotection accompanied by a simultaneous bis‐spiroacetalisation as a key step.
ChemInform Abstract: Bioactivity‐Guided Isolation of Mosquitocidal Constituents from the Rhizomes of Plumbago capensis Thunb
Authors: Sreelatha T. , Hymavathi A. , Murthy J. Madhusudhana , Rani P. U. , Rao J. Madhusudana , Babu K. Suresh
Published: September 2010

isolation and structure elucidation of two new naphthoquinone derivatives with moderate mosquitocidal activity, isoplumbagolone (I) and chitranane (II), along with other known compounds possessing potent larvicidal potentials
ChemInform Abstract: Ultrathin PbS Sheets by Two‐Dimensional Oriented Attachment.
Authors: Weller Horst , et al. et al.
Published: September 2010

Chlorine‐containing co‐solvents can direct the colloidal synthesis of PbS nanoparticles into two‐dimensional nanosheets by oriented attachment.
ChemInform Abstract: Discovery of Antiinflammatory Clinical Candidate E6201, Inspired from Resorcylic Lactone LL‐Z1640‐2, III.
Authors: Wang Yuan , et al. et al.
Published: September 2010

Nitrogen analogues of type (I) and (II) of the known resorcylic lactone LL‐Z1640‐2 are prepared.
ChemInform Abstract: Novel Tetracyclic Imidazole Derivatives: Synthesis, Dynamic NMR Study, and Antiinflammatory Evaluation.
Authors: Rupcic Renata , Modric Marina , Hutinec Antun , Cikos Ana , Stanic Barbara , Mesic Milan , Pesic Dijana , Mercep Mladen
Published: September 2010

A multistep route provides access to tetracyclic imidazoles such as (I) and (II).
ChemInform Abstract: Synthesis and Antihepatitis C Virus Activity of Morpholino Triazine Derivatives.
Authors: Misawa Takashi , Salim Mohammed T. A. , Okamoto Mika , Baba Masanori , Aoyama Hiroshi , Hashimoto Yuichi , Sugita Kazuyuki
Published: September 2010

A series of 18 title compounds of type (I) is prepared by usual organic synthetic methods.
ChemInform Abstract: 1‐(2‐Ethoxyethyl)‐1H‐pyrazolo[4,3‐d]pyrimidines as Potent Phosphodiesterase 5 (PDE5) Inhibitors.
Authors: Tollefson Michael B. , Acker Brad A. , Jacobsen E. J. , Hughes Robert O. , Walker John K. , Fox David N. A. , Palmer Michael J. , Freeman Sandra K. , Yu Ying , Bond Brian R.
Published: September 2010

A series of 32 title compounds are prepared and tested as phosphodiesterase 5 (PDE5) inhibitors.
ChemInform Abstract: Ion Dynamics at Interfaces: Nuclear Magnetic Resonance Studies
Authors: Heitjans Paul , Wilkening Martin
Published: September 2010

Review: 119 refs.
ChemInform Abstract: Mixed‐Valence Manganites
Authors: Coey J. M. D. , Viret M. , von Molnar S.
Published: September 2010

Review: 603 refs.
ChemInform Abstract: Growth Opportunities with Soft Magnetic Materials
Authors: Narasimhan Kalathur , Hanejko Francis , Marucci Michael L.
Published: September 2010

Review: 15 refs.
ChemInform Abstract: Advances in Soft Magnetic Composites ‐ Materials and Applications
Authors: Andersson Ola , Hofecker Paul
Published: September 2010

Review: 6 refs.
ChemInform Abstract: Specific Features of Spin, Charge, and Orbital Ordering in Cobaltites
Authors: Ivanova N. B. , Ovchinnikov S. G. , Korshunov M. M. , Eremin I. M. , Kazak N. V.
Published: September 2010

Review: 299 refs.
ChemInform Abstract: Surface Science as a Tool for Probing Nanocatalysis Phenomena
Authors: Vinod C. P.
Published: September 2010

Review: 59 refs.
ChemInform Abstract: Synthesis and Stabilization — Advances in Organoalkaline Earth Metal Chemistry
Authors: Buchanan William D. , Allis Damian G. , Ruhlandt‐Senge Karin
Published: September 2010

Review: 181 refs.
ChemInform Abstract: Metal Complexes as Protein Kinase Inhibitors
Authors: Kunick Conrad , Ott Ingo
Published: September 2010

Review: iridium complexes; 13 refs.
ChemInform Abstract: Supramolecular Gels as Active Media for Organic Reactions and Catalysis
Authors: Escuder Beatriu , Rodriguez‐Llansola Francisco , Miravet Juan F.
Published: September 2010

Review: more than 120 refs.
ChemInform Abstract: Fluorous Linker Units
Authors: Zhang Wei
Published: September 2010

Review: 101 refs.
ChemInform Abstract: Boron and Stannane Linker Units
Authors: Scott Peter J. H.
Published: September 2010

Review: 84 refs.
ChemInform Abstract: Selenium‐ and Tellurium‐Based Linker Units
Authors: But Tracy Yuen Sze , Toy Patrick H.
Published: September 2010

Review: 75 refs.
ChemInform Abstract: Diversity Cleavage Strategies from Phosphorus Linkers
Authors: Steel Patrick G. , Woods Tom M.
Published: September 2010

Review: 46 refs.
ChemInform Abstract: Hydrazone Linker Units
Authors: Lazny Ryszard
Published: September 2010

Review: 31 refs.
ChemInform Abstract: T1 and T2: Versatile Triazene Linker Groups
Authors: Knepper Kerstin , Ziegert Robert E.
Published: September 2010

Review: 81 refs.
ChemInform Abstract: Introduction to Diversity‐Oriented Synthesis
Authors: Spandl Richard J. , Thomas Gemma L. , Diaz‐Gavilan Monica , O'Connell Kieron M. G. , Spring David R.
Published: September 2010

Review: 70 refs.
ChemInform Abstract: Enzyme Cleavable Linker Units
Authors: Bejugam Mallesham , Flitsch Sabine L.
Published: September 2010

Review: 48 refs.
ChemInform Abstract: Nucleophile Cleavable Linker Units
Authors: Porcheddu Andrea , Giacomelli Giampaolo
Published: September 2010

Review: 138 refs.
ChemInform Abstract: Management Guidelines for the Use of Alemtuzumab in Chronic Lymphocytic Leukemia
Authors: Oesterborg A. , Foa R. , Bezares R. F. , Dearden C. , Dyer M. J. S. , Geisler C. , Lin T. S. , Montillo M. , van Oers M. H. J. , Wendtner C.‐M. , et al. et al.
Published: September 2010

Review: 67 refs.
ChemInform Abstract: Aromaticity and Photophysical Properties of Various Topology‐Controlled Expanded Porphyrins
Authors: Shin Jae‐Yoon , Kim Kil Suk , Yoon Min‐Chul , Lim Jong Min , Yoon Zin Seok , Osuka Atsuhiro , Kim Dongho
Published: September 2010

Review: 50 refs.
ChemInform Abstract: Nucleophilic Substitution of Hydrogen in Electron‐Deficient Arenes, a General Process of Great Practical Value
Authors: Makosza Mieczyslaw
Published: September 2010

Review: ca. 80 refs.
ChemInform Abstract: The First Artificial Cell — A Revolutionary Step in Synthetic Biology?
Authors: Bornscheuer Uwe T.
Published: September 2010

Review: 14 refs.
ChemInform Abstract: Natural Products as Antifungal Agents Against Clinically Relevant Pathogens
Authors: Di Santo Roberto
Published: September 2010

Review: 124 refs.
ChemInform Abstract: Involvement of Glycemic Control in the Inhibiting Effect of Morinda citrifolia on Cerebral Ischemia‐Induced Neuronal Damage
Authors: Harada Shinichi , Fujita‐Hamabe Wakako , Kamiya Kohei , Satake Toshiko , Tokuyama Shogo
Published: September 2010

Review: 31 refs.
ChemInform Abstract: Donepezil‐Induced Neuroprotection of Acetylcholinergic Neurons in Olfactory Bulbectomized Mice
Authors: Yamamoto Yui , Shioda Norifumi , Han Feng , Moriguchi Shigeki , Fukunaga Kohji
Published: September 2010

Review: 34 refs.
ChemInform Abstract: Design of Phase‐Vanishing Reactions
Authors: Van Zee Nathan J. , Dragojlovic Veljko
Published: September 2010

Review: 40 refs.
ChemInform Abstract: Application of Iridium Catalysts in the Fine Chemicals Industry
Authors: Blaser Hans‐Ulrich
Published: September 2010

Review: 46 refs.
ChemInform Abstract: Formulation and Characterisation of Hot Melt Extruded Dosage Forms: Challenges and Opportunities
Authors: Jones David S. , Andrews Gavin P.
Published: September 2010

Review: 9 refs.
ChemInform Abstract: The Activation Strain Model of Chemical Reactivity
Authors: van Zeist Willem‐Jan , Bickelhaupt F. Matthias
Published: September 2010

Review: about 80 refs.
ChemInform Abstract: Mathematical Modelling of the Decomposition of Explosives
Authors: Smirnov L. P.
Published: September 2010

Review: 168 refs.
ChemInform Abstract: The Past, Present and Future of Enzyme Measurements Using Surface Enhanced Raman Spectroscopy
Authors: Larmour Iain A. , Faulds Karen , Graham Duncan
Published: September 2010

Review: 81 refs.
ChemInform Abstract: Extraction Behavior of Metal Cations with Calixarene Derivatives
Authors: Ohto Keisuke
Published: September 2010

Review: 84 refs.
Use of Diamond Electrodes for the Production of Service Water by Electrochemical Disinfection of Biologically Treated Waste Water
Authors: Dittmar T. , Haaken D. , Schmalz V. , Worch E.
Published: September 2010

Die direkte Wiederverwendung von Abwässern erfordert aufgrund der Infektionsgefahr durch pathogene Keime deren Desinfektion. Neben Membranfiltration und UV‐Behandlung könnte die elektrochemische Desinfektion hierfür eine geeignete Alternative darstellen. Die Anwendung von Diamantelektroden im Bereich der Abwasserdesinfektion wurde in Abhängigkeit von wichtigen Betriebs‐ und Abwasserparametern untersucht.
Kinetics of Anaerobic Biodegradation of Glycerol by Sulfate‐Reducing Bacteria
Authors: Dinkel W. , Frechen F.‐B. , Kljavlin M. S.
Published: September 2010

Die Wirtschaftlichkeit der Produktion von Biosulfid für die Schwermetall‐ oder Sulfatelimination aus Industrieabwässern hängt ausschlaggebend vom verwendeten Substrat ab und steht in direktem Zusammenhang mit der Verwertbarkeit der Kohlenstoffquelle durch Mikroorganismen. Leicht zugänglich und einfach in der Handhabung ist Glycerin als Substrat für die sulfatreduzierenden Bakterien (SRB). Gegenstand der hier vorgestellten Arbeiten war die Untersuchung des anaeroben Glycerinabbaus in der Batch‐Fermentation mithilfe einer Mischkultur von SRB und die Ermittlung eines kinetischen Modellansatzes.
Synthesis, Crystal Structure and Piezoelectric Property of Noncentrosymmetric Compound with Betti Base
Authors: Zhang Yuan , Han Mengting , Ye Qiong , Xiong Rengen
Published: September 2010

The molten reaction of 2‐naphthol, 2‐hydroxybenzaldehyde and tetrahydropyrrole at about 120°C yields 1‐[(2‐hydroxyphenyl)(pyrrolidin‐1‐yl)‐methyl]naphthalen‐2‐ol, whose co‐crystal (1) with 2‐naphthol was characterized by X‐ray single crystal diffraction, XRPD and IR. Compound 1 crystallizes in a noncentrosymmetric space group (Fdd2) with unit cell dimensions of a=2.9395(9) nm, b=3.468(3) nm, c=0.8013(8) nm, V=8.170(13) nm3, α=β=γ=90.0° and Z=8 [at 293(2) K]. The piezoelectric measurement result shows compound 1 is piezoelectrically active material with d33 value of ca. 6.2 pC/N. Temperature‐ and frequency‐dependent dielectric constant of compound 1 were measured and showed no distinct dielectric anomaly, which suggest no phase transition within the measured temperature range (100–410 K).
Theoretical Investigation on the Mechanism and Design of Catalysts for Nitrolysis of Hexamine
Authors: Shi Liangwei , Zhao Gang , Zhang Yazhu , Zheng Changwu , Qin Guangming , Lü Jian
Published: September 2010

The mechanism of nitrolysis of hexamine (HA) by DFT method has been explored to understand the classical organic reaction and assist the design of new catalyst. The potential energy surface of NO+2 was firstly investigated. A reasonable configuration evolution of NO+2 during the process of its reaction with HA was figured out. The role of H+ and NH+4 for the nitrolysis of HA was analyzed and discussed. The route of nitrolysis reaction from HA to 1‐acetoxylmethene‐3‐nitro‐tetrazabicyclo[3,3,1]nonane intermediate is similar to that of acetylation of HA. The relative free energy calculation proves the priority of nitrolysis relative to acetylation. Two types of Lewis salts, M(OSO2CF3)3 and M[N(SO2CF3)2]3 (M: Yb, Sm, Y, and Eu), are designed on the basis of discussed mechanism. The calculation for the key bond order in IM2[CH2R] model intermediates gives an indicator as the preferable catalyst. The experimental results support the theoretical conclusion.
Construction and Biofunction of 3‐Dimensional Self‐assembly Collagen Nanostructure on PLLA Substrate
Authors: Xu Shouhong , Liu Aiping , Lin Xiaoxiao , Liu Honglai , Yonese Masakastu
Published: September 2010

A 3‐dimensional and multi‐layered network nanostructure of collagen assembled on the poly(L‐lactic) acid (PLLA) substrate was reported. Collagen adsorption layers were prepared by dipping PLLA substrates into collagen solutions with various pH. The influences of adsorption interval, pH of collagen solutions and properties of PLLA substrate on the adsorption behavior of collagen were investigated by using atomic force microscopy and ellipsometry measurements. It was found that the multiple association degrees of collagen molecules in solution at a certain pH value seemed to play an important role in the adsorption process. The distinct adsorption behavior determined a specific 3‐dimensional structure formed at the interface. Furthermore, calcium carbonate (CaCO3) can be biomimetically crystallized by the inducement of biomineralization on these collagen layers.
The [2+2]‐Cycloaddition Reaction of Bisallenes: A Dramatic Substituent Effect
Authors: Lu Ping , Ma Shengming
Published: September 2010

The bisallenes 1 possessing a phenylsulfonyl or n‐butyl substituent at the internal position of allene moieties could be smoothly transformed to the bicyclo[5.2.0] or bicyclo[6.2.0] derivatives 2 in moderate to excellent yields with good regioselectivity upon refluxing in toluene. This [2+2]‐cycloaddition reaction shows an interesting substituent effect as unveiled by comparing with the results of unsubstituted substrates. However, further attention should be paid to the control of the regioselectivity of the [2+2]‐cycloaddition involving different CC bonds.
CuBr/N,N‐Dimethylglycine‐Catalyzed Coupling Reaction of 2‐Chlorotrifluoroacetanilides with Phenols at Mild Conditions
Authors: Hao Chao , Zhang Yihua , Jiang Yongwen , Ma Dawei
Published: September 2010

The ortho‐substituent effect directed by the CF3CONH group exists in CuBr/N,N‐dimethylglycine‐catalyzed diaryl ether formation from o‐chlorotrifluoroacetanilides and phenols, leading to this coupling reaction proceeding at 80°C to afford a wide range of diaryl ethers. The halogen‐exchange also plays an important role in this transformation because adding potassium iodide is essential for complete conversion.
Synthesis of Functionalized γ‐Lactams via Copper‐Catalyzed Intramolecular C‐Vinylation of Activated Methylene Compounds
Authors: Chen Liqun , Shi Min , Li Chaozhong
Published: September 2010

With the catalysis of CuI/3,4,7,8‐tetramethyl‐1,10‐phenanthroline, a number of N‐(2‐iodoallyl)‐2‐(ethoxycarbonyl)alkanamides underwent efficient intramolecular C‐vinylation in THF at 50°C leading to the synthesis of functionalized γ‐lactams in 61% –99% yields.
The Chemistry of Open‐cage Fullerene, Hydroxylamine Mediated Hole‐closing and ‐opening Reactions
Authors: Zhang Jianxin , Yang Dazhi , Xiao Zuo , Gan Liangbing
Published: September 2010

The fullerene‐mixed peroxide C60(O)(OOt‐Bu)6 was found to react with FeCl3 to form open‐cage compounds C60(O)4(OOt‐Bu)4 2 and C60(O)2(OH)(OOt‐Bu)5 3. Addition of hydroxyl amine to 3 closes the opening, yielding compound 5 with a hemiacetal and hemiaminal moiety. Oxidation of 5 with diacetoxyliodobenzene eliminates the hydroxylamine addend and reforms the open‐cage compound 3.
Synthesis of Bisazacalix[n]pyridines and Their Complexation with C60 and C70
Authors: Zhang Enxuan , Wang Dexian , Huang Zhitang , Wang Meixiang
Published: September 2010

Disulfane‐linked bisazacalix[n]pyridines (n=4, 7) were synthesized for the first time using a macrocyclic fragment coupling approach followed by post‐macrocyclization photoreaction with ethanethioic acid and hydrolysis under basic conditions. The bis‐macrocyclic compounds acted as strong receptors to form 1:1 complex with C60 and C70, giving a binding constant (Ka(1:1)) up to 107000 L·mol−1. The cooperation of two mono‐macrocyclic improved binding affinity to fullerenes.
Enantioselective Synthesis of the Diazatricyclic Core of Alkaloid TAN1251C via an Iodoaminocyclization Reaction
Authors: Zhang Hongkui , Lin Zhijie , Huang Huang , Huo Haohua , Huang Yanju , Ye Jianliang , Huang Peiqiang
Published: September 2010

A concise enantioselective synthesis of the diazatricyclic core of alkaloid TAN1251C is reported. The method featured a stereoselective formation of the iodide intermediate 16b (in 2:1 ratio) from homoallylic amine 11b by iodine‐promoted iodoaminocyclization, a previously claimed to be unsuccessful reaction. The intermediate 16b was converted to the tricyclic core of TAN1251C 28 in five steps. During this study, two unexpected products 22 and 25 were obtained, and compound 23, derived from 11a was shown to be unsuitable for the oxidative formation of the enamide of TAN1251C.
Synthesis of Talosin A and B, Two Bioactive Isoflavonoid Glycosides
Authors: Wu Zhongtao , Lian Gaoyan , Yu Biao , Wang Zhenzhong , Zhao Yiwu , Xiao Wei
Published: September 2010

Talosin A and B, namely genistein 7‐O‐α‐L‐6‐deoxy‐talopyranoside and genistein 4′,7‐di‐O‐α‐L‐6‐deoxy‐talopyranoside, which show excellent antifungal and anti‐inflammatory activities, were synthesized concisely.
Charge‐Transfer Effect on Chiral Phosphoric Acid Catalyzed Asymmetric Baeyer‐Villiger Oxidation of 3‐Substituted Cyclobutanones Using 30% Aqueous H2O2 as the Oxidant
Authors: Xu Senmiao , Wang Zheng , Zhang Xumu , Ding Kuiling
Published: September 2010

The intermolecular charge‐transfer effect has been employed for the first time as a modulating approach to affect the enantioselectivity in asymmetric catalysis by taking the chiral phosphoric acid catalyzed asymmetric Baeyer‐Villiger oxidation of 3‐aryl cyclobutanones as the reaction prototype. It was found that the electron acceptor additives were able to effectively tune the enantioselectivity via donor‐acceptor interaction with the catalyst and up to 9% enhancement of ee value was observed in a favorable case.
A 2,2′‐Bipyridyl‐Bridged Tetrathiafulvalene‐quinone Dyad: Intramolecular Electron‐Transfer Promoted by Metal Ions
Authors: Huang Guangxi , Zhang Deqing , Zhang Guanxin , Zhu Daoben
Published: September 2010

A 2,2′‐bipyridyl‐bridged tetrathiafulvalene (TTF)‐quinone dyad (1) was synthesized and characterized. Both absorption and ESR spectroscopic studies clearly indicate that electron transfer occurs from TTF to the quinone unit for dyad 1 in the presence of metal ions. The results manifest that the coordination of dyad 1 with metal ions plays a key role in facilitating the intramolecular electron transfer.
Design, Synthesis and Insecticidal Evaluation of Novel Pyrazolecarboxamides Containing Cyano Substituted N‐Pyridylpyrazole
Authors: Liu Zhili , Feng Qi , Xiong Lixia , Wang Mingzhong , Li Zhengming
Published: September 2010

12 novel pyrazolecarboxamides containing cyano substituted N‐pyridylpyrazole were synthesized, and their structures were characterized by 1H NMR and HRMS techniques. Their evaluated insecticidal activities against oriental armyworm (Mythimna separata) indicated that the cyano‐containing pyrazolecarboxamides exhibited moderate insecticidal activities. Compounds 6i and 6k showed comparable higher activity than corresponding anthranilic diamide 6m.
Cu‐Catalyzed Asymmetric Michael Addition of Glycine Derivatives to α,β‐Unsaturated Malonates
Authors: Hou Xuelong , Li Qing , Yao Jun , Dai Lixin
Published: September 2010

Michael addition of glycine imines with alkylidene and arylidene malonates has been developed using Cu/FcPhox as catalyst, providing corresponding Michael products in high yields with high diastereo‐ and enantioselectivities.
Studies of the Interesting Gas‐phase Rearrangement Reactions of 2‐Pyrimidinyloxy‐N‐arylbenzylurea Promoted by Urea‐Carbamimidic Acid Tautomerism by ESI‐MS/MS and Theoretical Computation
Authors: Xu Chu , Wang Haoyang , Zhao Zhixiong , Tang Qinghong , Guo Yinlong , Lü Long
Published: September 2010

The gas‐phase rearrangement reactions of compound 1, 2‐dimethoxypyrimidinyloxybenzylaminoben‐ zenedipropylurea, were studied by ESI‐MS/MS. The experimental results showed that introduction of dipropylurea moiety into the molecule initiated various interesting gas‐phase chemistries and the mechanisms were proposed on the basis of hydrogen/deuterium (H/D) exchange experiments and theoretical computations. Moreover, product 2, the solution‐phase rearrangement product of compound 1, was synthesized and its gas‐phase chemistries were also studied to support the propos gas‐phase rearrangement reactions of compound 1.
Conversion of Glucose in CPL‐LiCl to 5‐Hydroxymethylfurfural
Authors: Chen Tianming , Lin Lu
Published: September 2010

5‐Hydroxymethylfurfural (HMF), an important versatile sugar derivative, is also considered a key intermediate between petroleum‐based industrial organic chemistry and bio‐based carbohydrate chemistry. Here, we report that caprolactam (CPL) containing lithium chloride (LiCl) is a privileged solvent that enables the synthesis of the renewable platform chemical 5‐hydroxymethylfurfural (HMF) from purified glucose. Metal halides in CPL‐LiCl are catalysts, among which CrCl3, CrCl2, SnCl4 and SnCl2 are found to be uniquely effective, leading to the conversion of glucose to HMF with yields of 55% –67%. The simplicity of this chemical transformation of glucose contrasts markedly with the complexity of extant processes and provides a new paradigm for the use of biomass as a raw material for a renewable energy and chemical industries.
A Highly Efficient and Selective Turn‐on Fluorescent Sensor for Cu2+ Ion
Authors: Wang Xuehua , Cao Jing , Chen Chuanfeng
Published: September 2010

A new fluorescent chemosensor based on an open‐chain azacrown bearing a quinoline subunit was conveniently synthesized, which showed a remarkable enhanced fluorescent intensity in the presence of Cu2+ ion and a high selectivity toward Cu2+ ion over a wide range of tested metal ions in acetonitrile.
Exon‐skipped dystrophins for treatment of Duchenne muscular dystrophy: Mass spectrometry mapping of most exons and cooperative domain designs based on single molecule mechanics
Authors: Krieger Christine Carag , Bhasin Nishant , Tewari Manorama , Brown Andre E. X. , Safer Daniel , Sweeney H. Lee , Discher Dennis E.
Published: September 2010

Force‐bearing linkages between the cytoskeleton and extracellular matrix are clearly important to normal cell viability—as is evident in a disease such as Duchenne muscular dystrophy (DMD) which arises in the absence of the linkage protein dystrophin. Therapeutic approaches to DMD include antisense‐mediated skipping of exons to delete nonsense mutations while maintaining reading frame, but the structure and stability of the resulting proteins are generally unclear. Here we use mass spectrometry to detect most dystrophin exons, and we express and physically characterize dystrophin “nano”‐constructs based on multiexon deletions that might find use in a large percentage of DMD patients. The primary structure challenge is addressed first with liquid chromatography tandem mass spectrometry (LC‐MS/MS) which can detect tryptic peptides from 53 of dystrophin's 79 exons; equivalent information from immunodetection would require 53 different high‐specificity antibodies. Folding predictions for the nano‐constructs reveal novel helical bundle domains that arise out of exon‐deleted “linkers,” while secondary structure studies confirm high helicity and also melting temperatures well above physiological. Extensional forces with an atomic force microscope nonetheless unfold the constructs, and the ensemble of unfolding trajectories reveal the number of folded domains, proving consistent with structure predictions. A mechanical cooperativity parameter for unfolding of tandem domains is also introduced as the best predictor of a multiexon deletion that is asymptomatic in humans. The results thereby provide insight and confidence in exon‐skipped designs. © 2010 Wiley‐Liss, Inc.
Pulmonary tuberculosis increases the risk of lung cancer
Authors: Wu Chen‐Yi , Hu Hsiao‐Yun , Pu Cheng‐Yun , Huang Nicole , Shen Hsi‐Che , Li Chung‐Pin , Chou Yiing‐Jeng
Published: September 2010

BACKGROUND:

The possible effect of pulmonary tuberculosis (TB) on subsequent lung cancer development has been suspected, but the evidence remains inconsistent. The purpose of this study was to perform a nationwide population‐based cohort study to investigate the risk of lung cancer after pulmonary TB infection.

METHODS:

This nationwide population‐based cohort study was based on data obtained from the Taiwan National Health Insurance Database. In total, 5657 TB patients and 23,984 controls matched for age and sex were recruited for the study from 1997 to 2008.

RESULTS:

The incidence rate of lung cancer (269 of 100,000 person‐years) was significantly higher in the pulmonary TB patients than that in controls (153 of 100,000 person‐years) (incidence rate ratio [IRR], 1.76; 95% confidence interval [CI], 1.33‐2.32; P < .001). Compared with the controls, the IRRs of lung cancer in the TB cohort were 1.98 at 2 to 4 years, 1.42 at 5 to 7 years, and 1.59 at 8 to 12 years after TB infections. The multivariate Cox proportional hazards model revealed pulmonary TB infections (hazard ratio [HR], 1.64; 95% CI, 1.24‐2.15; P < .001) and chronic obstructive pulmonary disease (HR, 1.09; 95% CI, 1.03‐1.14; P = .002) to be independent risk factors for lung cancer.

CONCLUSIONS:

Pulmonary infection with TB is associated with an increased risk of lung cancer. Cancer 2011. © 2010 American Cancer Society.