bluuebunny/crossref_metadata_2025 huggingface dataset:
Biodegradable poly(glycolic acid) nanofiber prepared by CO2 laser supersonic drawing
Authors: Suzuki Akihiro , Shimizu Rio
Published: March 2011

Biodegradable Poly(glycolic acid) (PGA) nanofibers were prepared by irradiating a PGA fiber with radiation from a carbon dioxide (CO2) laser while drawing it at supersonic velocities and was collected as a nonwoven. A supersonic jet was generated by blowing air into a vacuum chamber through the fiber injection orifice. The flow velocity from the orifice was estimated by computer simulation; the fastest flow velocity was calculated to be 401 m s−1 at a chamber pressure of 6 kPa. A nanofiber obtained using a laser power of 10 W and a chamber pressure of 6 kPa had an average diameter of 359 nm and a draw ratio of about 77,600. © 2011 Wiley Periodicals, Inc. J Appl Polym Sci, 2011
Anatomy of the failure rate: A mathematical dissection
Authors: Singpurwalla Nozer D.
Published: March 2011

The failure rate function is one of the most commonly used notion in reliability engineering and in survival analysis. The purpose of this expository paper is to point out some mathematical issues connected with this notion, a consequence of which is that under certain circumstances the famous exponentiation formula overestimates the probability of survival. To demonstrate this we point out a scenario that results in Volterra's product integrals, instead of the usual Lebesgue integral for which the exponentiation formula is exact. Copyright © 2011 John Wiley & Sons, Ltd.
Altered substrate specificity of the gluco‐oligosaccharide oxidase from Acremonium strictum
Authors: Foumani Maryam , Vuong Thu V. , Master Emma R.
Published: March 2011

A gluco‐oligosaccharide oxidase (GOOX) from Acremonium strictum type strain CBS 346.70 was cloned and expressed in Pichia pastoris. The recombinant protein, GOOX‐VN, contained fifteen amino acid substitutions compared with the previously reported A. strictum GOOX. These two enzymes share 97% sequence identity; however, only GOOX‐VN oxidized xylose, galactose, and N‐acetylglucosamine. Besides monosaccharides, GOOX‐VN oxidized xylo‐oligosaccharides, including xylobiose and xylotriose with similar catalytic efficiency as for cello‐oligosaccharides. Of three mutant enzymes that were created in GOOX‐VN to improve substrate specificity, Y300A and Y300N doubled kcat values for monosaccharide and oligosaccharide substrates. With this novel substrate specificity, GOOX‐VN and its variants are particularly valuable for oxidative modification of cello‐ and xylo‐oligosaccharides. Biotechnol. Bioeng. 2011;108: 2261–2269. © 2011 Wiley Periodicals, Inc.
Removal and recovery of furfural, 5‐hydroxymethylfurfural, and acetic acid from aqueous solutions using a soluble polyelectrolyte
Authors: Carter Brian , Gilcrease Patrick C. , Menkhaus Todd J.
Published: March 2011

In the cellulosic ethanol process, furfural, 5‐hydroxymethylfurfural (HMF), and acetic acid are formed during the high temperature acidic pretreatment step needed to convert biomass into fermentable sugars. These compounds can inhibit cellulase enzymes and fermentation organisms at relatively low concentrations (≥1 g/L). Effective removal of these inhibitory compounds would allow the use of more severe pretreatment conditions to improve sugar yields and lead to more efficient fermentations; if recovered and purified, they could also be sold as valuable by‐products. This study investigated the separation of aldhehydes (furfural and HMF) and organic acid (acetic acid) inhibitory compounds from simple aqueous solutions by using polyethyleneimene (PEI), a soluble cationic polyelectrolyte. PEI added to simple solutions of each inhibitor at a ratio of 1 mol of functional group to 1 mol inhibitor removed up to 89.1, 58.6, and 81.5 wt% of acetic acid, HMF, and furfural, respectively. Furfural and HMF were recovered after removal by washing the polyelectrolyte/inhibitor complex with dilute sulfuric acid solution. Recoveries up to 81.0 and 97.0 wt% were achieved for furfural and HMF, respectively. The interaction between PEI and acetic acid was easily disrupted by the addition of chloride ions, sulfate ions, or hydroxide ions. The use of soluble polymers for the removal and recovery of inhibitory compounds from biomass slurries is a promising approach to enhance the efficiency and economics of an envisioned biorefinery. Biotechnol. Bioeng. 2011;108:2046–2052. © 2011 Wiley Periodicals, Inc.
Effects of miR‐541 on neurite outgrowth during neuronal differentiation
Authors: Zhang Jun , Zhang Jing , Liu Li‐hong , Zhou Yang , Li Yi‐ping , Shao Zhi‐hua , Wu You‐jun , Li Meng‐jie , Fan Ying‐ying , Shi Hong‐jun
Published: March 2011

MicroRNA (miRNAs) are short non‐coding RNA molecules that downregulate gene expression at post‐transcriptional level. miRNAs are post‐transcriptional regulators of gene expression important for neuron development and function. This report demonstrated that a putative and chemically synthesized miRNA rno‐mir‐541 played an important role in the neuron development. Differentiation of PC12 cells with nerve growth factor (NGF) is associated with neurite outgrowth, a process that involves upregulation of Synapsin I. We predicted, detected and assessed the expression levels of a number of possible miRNAs for synapsin I in rats and our outcomes showed that rno‐mir‐541 was associated with rat synapsin I expression. miR‐541, a brain specific miRNA, plays an important role in repressing neurite extension in cultured PC12 neurons. The neurites of PC12 cells was shortened drasticly as a result of the overexpression of rno‐mir‐541. In contrast, the neurites of PC12 cell developed well after the knockdown of rno‐mir‐541 by RNA interference. Our study showed that rno‐mir‐541 played an important role in neuron‐cell proliferation and neurite outgrowth through suppressing the expression of its target gene synapsin I. Furthermore, the introduction of NGF causes downregulation of miR‐541, de‐repression of its target, Synapsin‐I and allows for neuritogenesis. Thus, miR‐541 functions in neuronal precursors as an endogenous conditional component between NGF and Synapsin‐I. Copyright © 2011 John Wiley & Sons, Ltd.
Enhancing β3‐Peptide Bundle Stability by Design
Authors: Craig Cody J. , Goodman Jessica L. , Schepartz Alanna
Published: March 2011

We reported recently that certain β3‐peptides self‐assemble in aqueous solution into discrete bundles of unique structure and defined stoichiometry. The first β‐peptide bundle reported was the octameric Zwit‐1F, whose fold is characterized by a well‐packed, leucine‐rich core and a salt‐bridge‐rich surface. Close inspection of the Zwit‐1F structure revealed four nonideal interhelical salt‐bridge interactions whose heavy atom–heavy atom distances were longer than found in natural proteins of known structure. Here we demonstrate that the thermodynamic stability of a β‐peptide bundle can be enhanced by optimizing the length of these four interhelical salt bridges. Combined with previous work on the role of internal packing residues, these results provide another critical step in the “bottom‐up” formation of β‐peptide assemblies with defined sizes, reproducible structures, and sophisticated function.
Stabilization of a Metabolic Enzyme by Library Selection in Thermus thermophilus
Authors: Schwab Thomas , Sterner Reinhard
Published: March 2011

The anthranilate phosphoribosyl transferase from the hyperthermophilic archaeon Sulfolobus solfataricus (sAnPRT, encoded by strpD), which catalyzes the third step in tryptophan biosynthesis, is a thermostable homodimer with low enzymatic activity at room temperature. We have combined two mutations leading to the monomerization and two mutations leading to the activation of sAnPRT. The resulting “activated monomer” sAnPRT‐I36E‐M47D+D83G‐F149S, which is much more labile than wild‐type sAnPRT, was stabilized by a combination of random mutagenesis and metabolic library selection using the extremely thermophilic bacterium Thermus thermophilus as host. This approach led to the identification of five mutations that individually increased the thermal stability of sAnPRT‐I36E‐M47D+D83G‐F149S by 1 to 8 °C, and by 13 °C when combined. The beneficial exchanges were located in different parts of the protein structure, but none of them led to the “re‐dimerization” of the enzyme. We observed a negative correlation between thermal stability and catalytic activity of the mutants; this suggests that conformational flexibility is required for catalysis by sAnPRT.
ChemInform Abstract: Crystal Structure of the Ag2SiS3 Compound.
Authors: Zhbankov O. , Fedorchuk A. , Kityk I. , Olekseyuk I. , Parasyuk O.
Published: March 2011

The title compound is synthesized by melting stoichiometric mixtures of the elements (quartz ampule, 1373 K, 6 h) followed by annealing at 673 K for 300 h.
ChemInform Abstract: Ca14Au46Sn5: A “Colored” Gd14Ag51‐Type Structure Containing Columns of Well‐Differentiated Hexagonal Gold Stars.
Authors: Lin Qisheng , Corbett John D.
Published: March 2011

Ca14Au46.67Sn4.14, Ca14Au45.79Sn4.94, and Ca14Au45.56Sn5.14 are synthesized by solid state reactions of the elements (850 °C, 24 h) and characterized by single crystal XRD.
ChemInform Abstract: Is Tl2Ni3S2 a Mixed Valent Compound? Crystal and Electronic Structure Investigations.
Authors: Bachhuber F. , Anusca I. , Rothballer J. , Pienlnhofer F. , Peter P. , Weihrich R.
Published: March 2011

The title compound is prepared from stoichiometric amounts of Tl2S2 and Ni (600 °C, 4 d) and characterized by single crystal XRD and DFT calculations.
ChemInform Abstract: The Effect of Strontium Deficiency in Pr0.6Sr0.4MnO3 Perovskite Manganites.
Authors: Koubaa W. Cheikhrouhou , Koubaa M. , Cheikhrouhou A.
Published: March 2011

The structural, magnetic, and magnetocaloric properties of Pr0.6Sr0.4‐δMnO3 (0 ≤ δ ≤ 0.2) are characterized by powder XRD and magnetic measurements.
ChemInform Abstract: 2D Zirconium Fluorides: Synthesis, Structure and NMR Spectroscopy.
Authors: Ben Ali A. , Body M. , Leblanc M. , Maisonneuve V.
Published: March 2011

Compounds (II) and (IV) are characterized by single crystal XRD and 19F NMR spectroscopy.
ChemInform Abstract: Synthesis, Crystal Structure and Property of a Novel Nickel‐Containing Tungstophosphate [Na3(H2O)8{Ni3(H2O) (B‐α‐PW9O34) (B‐β‐PW8O31)}2]21‐.
Authors: Chu Lili , Zhou Baibin , Wang Chunxiao , Zhao Zhifeng , Su Zhanhua , Yu Kai
Published: March 2011

Na21 [Na3(H2O)8{Ni3(H2O) (PW9O34) (PW8O31)}2]·36H2O is synthesized from an aqueous solution of Na2WO4, Na2HPO4, NiCl2, HCl, and NaOH (pH 6—7, 80 °C, 2 h, 46% yield).
ChemInform Abstract: Self‐Assembly of Supramolecular Networks Based on Biphosphopentamolybdate and Copper—Organic Units.
Authors: Su Zhanhua , Zhao Zhifeng , Zhou Baibin , Cai Qinghai , Wang Qun
Published: March 2011

The crystal structures of compounds (III) and (IV) are characterized by single crystal XRD.
ChemInform Abstract: 1,3‐Dibromo‐5,5‐dimethylhydantoin as an Efficient Homogeneous Catalyst for Synthesis of Benzoxazoles, Benzimidazoles, and Oxazolo[4,5‐b]pyridines.
Authors: Hojati Seyedeh Fatemeh , Maleki Behrooz , Beykzadeh Zahra
Published: March 2011

The condensation of orthoesters (II) with substituted anilines (I) and (IV) or aminohydroxypyridine (VI) is performed in the presence of the title catalyst under solvent‐free conditions to afford the corresponding heterocycles in good to excellent yields.
ChemInform Abstract: Solvent Free Oxidation of Primary Alcohols and Diols Using Thymine Iron(III) Catalyst.
Authors: Al‐Hunaiti Afnan , Niemi Teemu , Sibaouih Ahlam , Pihko Petri , Leskelae Markku , Repo Timo
Published: March 2011

An efficient and selective Fe‐based system for the synthesis of carboxylic acids (II) from primary alcohols (I) and ketones (IV) from secondary alcohols (III) is developed.
ChemInform Abstract: The Reaction of Cyclic Imines with the Ruppert—Prakash Reagent. Facile Approach to α‐Trifluoromethylated Nornicotine (IIIh), Anabasine (Vc), and Homoanabasine (Vf).
Authors: Shevchenko Nikolay E. , Vlasov Katja , Nenajdenko Valentine G. , Roeschenthaler Gerd‐Volker
Published: March 2011

Cyclic imines bearing α‐alkyl or (hetero)aryl groups are efficiently α‐trifluoromethylated.
ChemInform Abstract: Ruthenium‐Catalyzed Cascade N‐ and C(3)‐Dialkylation of Cyclic Amines with Alcohols Involving Hydrogen Autotransfer Processes.
Authors: Sundararaju Basker , Tang Zhou , Achard Mathieu , Sharma Gangavaram V. M. , Toupet Loic , Bruneau Christian
Published: March 2011

Pyrrolidine, piperidine, and azepane undergo the unprecedented title reaction with benzyl alcohols as well as an aliphatic alcohol in the presence of (p‐cymene)ruthenium(II) precatalyst RUT.
ChemInform Abstract: Palladium‐Catalyzed Coupling Reaction of α‐Diazocarbonyl Compounds with Aromatic Boronic Acids or Halides.
Authors: Peng Cheng , Yan Guobin , Wang Yan , Jiang Yubo , Zhang Yan , Wang Jianbo
Published: March 2011

The title process allows the synthesis of various α‐aryl substituted α,β‐unsaturated carbonyl compounds.
ChemInform Abstract: Lithium Naphthalenide Induced Reductive Alkylation and Addition of Aryl‐ and Heteroaryl‐Substituted Dialkylacetonitriles.
Authors: Tsao Jing‐Po , Tsai Ting‐Yueh , Chen I‐Chia , Liu Hsing‐Jang , Zhu Jia‐Liang , Tsao Sheng‐Wei
Published: March 2011

Treatment of trisubstituted acetonitriles with lithium naphthalenide results in a reductive decyanation.
ChemInform Abstract: Acetoxypalladation of Unactivated Alkynes and Capture with Alkenes to Give 1‐Acetoxy‐1,3‐dienes Taking Dioxygen as Terminal Oxidant.
Authors: Zhou Peng , Jiang Huanfeng , Huang Liangbin , Li Xianwei
Published: March 2011

A new and general method for the synthesis of the title dienes using an acetoxy‐palladation/Heck cross‐coupling/β‐H elimination tandem process is developed.
ChemInform Abstract: Microwave‐Assisted Domino Hydroformylation Without Syngas.
Authors: Cini Elena , Airiau Etienne , Girard Nicolas , Mann Andre , Salvadori Jessica , Taddei Maurizio
Published: March 2011

A convenient procedure is developed for domino hydroformylation cyclization reactions of unsaturated alcohols, amines and amides to produce various O‐ and N‐containing heterocycles.
ChemInform Abstract: Csp3—Csp2 Palladium‐—Catalyzed Cross‐Coupling Reaction of Trialkylbismuth Reagents with Aryl, Heteroaryl, and Vinyl Halides and Triflates.
Authors: Gagnon Alexandre , Albert Vincent , Duplessis Martin
Published: March 2011

The method does not require isolation of the trialkylbismuth species, which are generated in situ from the corresponding Grignard reagents and allows the transfer of primary alkyl groups having hydrogen atoms in the β‐position.
ChemInform Abstract: Phenyliodine Diacetate Mediated Oxidative Cleavage of Cyclobutanols Leading to γ‐Hydroxy Ketones.
Authors: Fujioka Hiromichi , Komatsu Hideyuki , Miyoshi Akihito , Murai Kenichi , Kita Yasuyuki
Published: March 2011

The 2‐substituted cyclobutanols (III) and (V) undergo regioselective cleavage.
ChemInform Abstract: Synthesis of 1,4‐Diazabutadienes (=N,N′‐Ethane‐1,2‐diylidenebis[amines]) by Grinding.
Authors: He Jingyu , Xin Hongxing , Yan Hong , Song Xiuqing , Zhong Rugang
Published: March 2011

1,4‐Diazabutadienes are easily synthesized by grinding glyoxal trimer dihydrate (I) or butanedione (IV) with anilines and catalytic amounts of TosOH under neat conditions.
ChemInform Abstract: The Use of Br/Cl to Promote Regioselective Gold‐Catalyzed Rearrangement of Propargylic Carboxylates: An Efficient Synthesis of (1Z,3E)‐1‐Bromo/Chloro‐2‐carboxy‐1,3‐dienes.
Authors: Wang Yanzhao , Lu Biao , Zhang Liming
Published: March 2011

An Au‐catalyzed synthesis of 1‐bromo/chloro‐2‐carboxy‐1,3‐dienes (II) and (VI) using propargylic carboxylates (I) and (V) containing halogenated alkynes as substrates is described.
ChemInform Abstract: Enantioselective Desymmetrization of Cyclopropenes by Hydroacylation.
Authors: Phan Diem H. T. , Kou Kevin G. M. , Dong Vy M.
Published: March 2011

Cyclopropylketones bearing vicinal tertiary and quaternary chiral centers are produced.
ChemInform Abstract: Ligand Influence in the Selective Gold‐Mediated Synthesis of Allenes.
Authors: Nun Pierrick , Gaillard Sylvain , Slawin Alexandra M. Z. , Nolan Steven P.
Published: March 2011

The use of [(IPr)AuOH] permits the generation of Au(I)‐amine complexes by a Ag‐free protocol.
ChemInform Abstract: Cs2CO3‐Mediated Synthesis of Terminal Alkynes from 1,1‐Dibromo‐1‐alkenes.
Authors: Zhao Ming , Kuang Chunxiang , Yang Qing , Cheng Xuezhi
Published: March 2011

The title reaction tolerates a wide range of functional groups.
ChemInform Abstract: First Application of Air‐Stable and Reusable Phosphine‐Containing Calix[4]arene in Catalytic Aza‐Morita—Baylis—Hillman Reaction.
Authors: Zhong Weihui , Zheng Yemin , Zhou Jiadi , Shen Yanyan
Published: March 2011

The phosphine substituent acts as Lewis base to initiate the title process and the hydroxy substituents act as Broensted acid to accelerate the reaction and to stabilize the transition state.
ChemInform Abstract: Synthesis and Application of Oxadiazines as Chiral Ligands for the Enantioselective Addition of Diethylzinc to Aldehydes.
Authors: Dean Melissa A. , Hitchcock Shawn R.
Published: March 2011

Oxadiazines (I) are prepared to be applied as catalysts in the title reaction.
ChemInform Abstract: A Simple Method for the Oxidation of Primary Alcohols with o‐Iodoxybenzoic Acid (IBX) in the Presence of Acetic Acid.
Authors: Lin Cheng‐Kun , Lu Ta‐Jung
Published: March 2011

A wide range of benzylic, allylic and aliphatic primary alcohols is efficiently oxidized by use of IBX—AcOH reagent system to give the aldehydes in up to 97% yield.
ChemInform Abstract: Synthesis of Novel Amides of Phenyl‐1,4‐dioxyacetic Acid as Molecular Tweezers and Studies on Their Molecular Recognition.
Authors: Li WeiJie , Zhao ZhiGang , Liu Xingli , Wang XiaoQing
Published: March 2011

A simple, efficient, and environmentally friendly method for the synthesis of the title compounds (V) is presented.
ChemInform Abstract: Catalytic Asymmetric Michael Reactions of α,β‐Unsaturated Ketones with Sulfonyl‐Containing Nucleophiles: Chiral Synthesis of (R)‐Muscone and (S)‐Celery Ketone.
Authors: Sun Xiaomin , Yu Feng , Ye Tingting , Liang Xinmiao , Ye Jinxing
Published: March 2011

Asymmetric Michael reaction between aliphatic (I) or alicyclic α,β‐unsaturated ketones (VII) and sulfonyl‐containing nucleophiles (II) and (IV) in the presence of an epi‐quinine‐derived organocatalyst provides the corresponding adducts in a highly enantioselective manner (up to 98% e.e.).
ChemInform Abstract: Direct Formation of α,β‐Unsaturated Dithioacetals from Diarylpropynols.
Authors: Curtis Ashley J. , Gabbutt Christopher D. , Heron B. Mark , Kilner Colin
Published: March 2011

Acid‐catalyzed condensation of diarylpyrroles with 2‐thionaphthol unexpectedly gives the title compounds (III) via a Meyer—Schuster‐type rearrangement.
ChemInform Abstract: Rh(III)‐Catalyzed Oxidative Coupling of Unactivated Alkenes via C—H Activation.
Authors: Tsai Andy S. , Brasse Mikael , Bergman Robert G. , Ellman Jonathan A.
Published: March 2011

A methoxy group in the oxime is essential to achieve high yields.
ChemInform Abstract: Synthesis of Biaryl Compounds Using Tandem Ruthenium‐Catalyzed Ring‐Closing Metathesis.
Authors: Yoshida Kazuhiro , Shida Hiroaki , Takahashi Hidetoshi , Yanagisawa Akira
Published: March 2011

A new method for the construction of various biaryl compounds is presented involving a tandem ring‐closing enyne metathesis and ring‐closing olefin metathesis of tetraenynes.
ChemInform Abstract: Diels—Alder Cycloaddition of o‐Quinonedimethides and Alkylidene‐5H‐furan‐2‐ones: New and Rapid Access to Lambertellol Cores and Arthrinone Derivatives.
Authors: Blanc Romain , Heran Virginie , Rahmani Raphael , Commeiras Laurent , Parrain Jean‐Luc
Published: March 2011

An efficient synthesis of deoxy‐lambertellols proceeds through a highly chemo‐ and diastereoselective Diels—Alder cycloaddition.
ChemInform Abstract: Preparation of Isoindolones by a Lithium—Iodide Exchange‐Induced Intramolecular Wurtz—Fittig Reaction of o‐Iodobenzoyl Chloride/Imine Adducts.
Authors: Campbell James B. , Dedinas Robert F. , Trumbower‐Walsh Sally
Published: March 2011

Addition of o‐iodobenzoyl chlorides to alkyl imines generates acyliminium ions which undergo phenyllithium‐induced intramolecular Wurtz—Fittig coupling to produce isoindolones.
ChemInform Abstract: A New Chiral Phoshine Oxide Ligand for Enantioselective 1,3‐Dipolar Cycloaddition Reactions of Azomethine Ylides.
Authors: Eroeksuez Serap , Dogan Oezdemir , Garner Philip P.
Published: March 2011

A variety of pyrrolidines is prepared with yields up to 97% and moderate to high enantioselectivities.
ChemInform Abstract: Smooth Photocatalytic Preparation of 2‐Substituted 1,3‐Benzodioxoles.
Authors: Ravelli Davide , Albini Angelo , Fagnoni Maurizio
Published: March 2011

Alkylation of a wide range of benzodioxoles at position 2 proceeds readily under photo‐induced conditions in the presence of (Bu4N)4W10O32 as photocatalyst.
ChemInform Abstract: Targeting Glycolysis: A Fragment Based Approach Towards Bifunctional Inhibitors of hLDH‐5.
Authors: Moorhouse Adam D. , Spiteri Christian , Sharma Pallavi , Zloh Mire , Moses John E.
Published: March 2011

Derivatives (V), synthesized via a fragment based “click” chemistry approach, demonstrate potent and selective inhibitory activity against human lactate dehydrogenase hLDH‐5.
ChemInform Abstract: Efficient One‐Pot Synthesis of Disubstituted 1,3,4‐Oxadiazole Derivatives from the Reaction of (N‐Isocyanimino)triphenylphosphorane, Acetaldehyde, a Secondary Amine, and an Electron‐Poor (E)‐Cinnamic Acid.
Authors: Ramazani Ali , Ahmadi Yavar , Tarasi Roghayeh
Published: March 2011

A plausible mechanism for this multicomponent reaction is provided.
ChemInform Abstract: Concise and Efficient Synthesis of 4‐Hydroxy‐2‐pyrones from Pentane‐2,4‐diones.
Authors: Yoshida Masahiro , Takai Hironobu , Mitsuhashi Chika , Shishido Kozo
Published: March 2011

The efficient, convenient, and practical synthesis is accomplished in two steps.
ChemInform Abstract: Preparation of Thioflavones via Thiophosphoryl Chloride Mediated Cyclodehydration and Thionation of 1‐(2‐Hydroxyphenyl)‐3‐arylpropane‐1,3‐diones.
Authors: Vimal Manorama , Pathak Uma , Pandey Lokesh Kumar , Suryanarayana Malladi V. S.
Published: March 2011

A simple one‐pot procedure allows the preparation of the title compounds via intermediate flavones.
ChemInform Abstract: Organocatalyzed Reactions Involving 3‐Formylchromones and Acetylenedicarboxylates: Efficient Synthesis of Functionalized Benzophenones and Polysubstituted Xanthones.
Authors: Terzidis Michael A. , Tsiaras Vassilios G. , Stephanidou‐Stephanatou Julia , Tsoleridis Constantinos A.
Published: March 2011

Reaction of 3‐formylchromones with diesters of type (II) gives xanthones (II) or benzophenones (V) depending on both on the nature of the chromone substituents and on the basicity of the organocatalyst.
ChemInform Abstract: Pyrrole Acylation for the Synthesis of 2‐Bromo‐6‐(2‐pyrrolyl)pyridine and Subsequent Cross‐Coupling Reactions.
Authors: Song Chuanjun , Liu Yan , Zhao Peng , Sun Xuelian , Li Wenjia , Liu Hui , Chang Junbiao
Published: March 2011

A previously developed pyrrole acylation process using carboxylic acids and TFAA is successfully applied as the initial step in the synthesis of the starting material (VII).
ChemInform Abstract: A Practical Procedure for the Removal of the Phenylethanol Moiety from Phenylglycinol‐Derived Lactams.
Authors: Semak Vladislav , Escolano Carmen , Arroniz Carlos , Bosch Joan , Amat Mercedes
Published: March 2011

The reaction proceeds without irradiation or catalysis with complete retention of configuration.
ChemInform Abstract: A Study of Antibacterial Activity of Some Novel 8‐Methoxy‐4‐methyl‐quinoline Derivatives.
Authors: Singh Sheoraj , Kumar Vikas , Kumar Ashok , Sharma Shalabh , Dua Piyush
Published: March 2011

Novel azetidinylamino‐ and thiazolidinylaminoquinolines are synthesized starting from quinolinol derivative (I), and evaluated in vitro for their antibacterial activity against gram positive bacteria.
ChemInform Abstract: Regioselective Introduction of Homoallylic Amine Moiety to Quinolines: Preparation of Reissert Compound Followed by In‐Mediated Allylation of Nitrile.
Authors: Kim Sung Hwan , Lee Sangku , Kim Yu Mi , Kim Jae Nyoung
Published: March 2011

Reissert compounds (I) are converted into homoallylic compounds (III) whereas the isoquinoline derived Reissert compound (IV) gives ring closure product (V) and N‐hexanoyl derivative (VI) unexpectedly yields imine (VII).
ChemInform Abstract: 4‐Hydroxy‐2‐quinolones. Part 179. Synthesis, Structure, and Antiinflammatory Activity of 4‐Hydroxy‐1‐methyl‐2‐oxo‐1,2‐dihydroquinolin‐3‐ylacetic Acid and Its Derivatives.
Authors: Ukrainets I. V. , Mospanova E. V. , Davidenko A. A. , Tkach A. A. , Gorokhova O. V.
Published: March 2011

9 Esters of type (V) are prepared and screened for their anti‐inflammatory activities.
ChemInform Abstract: Conjugate Addition — SNAr Domino Reaction for the Synthesis of Benzo‐ or Pyridyl‐Fused Lactams and Sultams.
Authors: Noerager Niels Groen , Juhl Karsten
Published: March 2011

The synthesis is achieved via addition of deprotonated amides, sulfonamides or hydrazines to ethyl propiolate derivatives (II) followed by nucleophilic substitution.
ChemInform Abstract: 3‐Methoxalylchromone — A Versatile Reagent for the Regioselective Synthesis of 1‐Desazapurine.
Authors: Ostrovskyi Dmytro , Iaroshenko Viktor O. , Ali Iftikhar , Mkrtchyan Satenik , Villinger Alexander , Tolmachev Andrei , Langer Peter
Published: March 2011

5‐Aminoimidazoles, prepared in situ from formimidate (II) and amines, react with title compound (I) to give the pharmaceutically important title skeleton (IV).
ChemInform Abstract: New Method for the Acetamination of Perimidines.
Authors: Aksenov A. V. , Aksenov N. A. , Nadein O. N. , Tsys' A. E.
Published: March 2011

The reaction is assumed to proceed via Beckmann rearrangement of intermediates (III).
ChemInform Abstract: Synthesis of 2,3,4‐Tri‐Substituted 3,4‐Dihydroquinazolines via Tandem Nucleophilic Addition/Epoxy Ring‐Opening Cyclization Methodology Using N‐(2‐Oxiranylphenyl)carbodiimides with Nucleophiles.
Authors: Saito Takao , Ote Tatsuya , Shiotani Masahiro , Kataoka Hiroko , Otani Takashi , Kutsumura Noriki
Published: March 2011

A variety of dihydroquinazolines are obtained diastereoselectively by reaction of carbodiimides (IX) with different O‐, S‐, N‐ and C‐nucleophiles.
ChemInform Abstract: Facile Synthesis of 1‐Methyl‐1H‐benzo[b]azepines from 1‐Methylquinolinium Iodides and Diazo(trimethylsilyl)methylmagnesium Bromide.
Authors: Morita Mikio , Hari Yoshiyuki , Aoyama Toyohiko
Published: March 2011

Starting from iodide (I), the synthesis of benzoazepines (IV) is achieved via addition of magnesium salt (II), followed by sequential Cu‐catalyzed ring expansion and desilylation.
ChemInform Abstract: Interaction of Derivatives of 7‐Amino‐1,5‐benzodiazepin‐2‐ones with α,β‐Unsaturated Ketones.
Authors: Janciene R. , Stumbreviciute Z. , Vektariene A. , Sirutkaitis R. , Podeniene D. , Palaima A. , Puodziunaite B.
Published: March 2011

Different products are obtained when diazepin‐2‐ones (I) or (VII) are reacted with α,β‐unsaturated carbonyl compounds (II) or (IV).
ChemInform Abstract: An Efficient Oxidative Dearomatization—Radical Cyclization Approach to Symmetrically Substituted Bicyclic Guttiferone Natural Products.
Authors: McGrath Nicholas A. , Binner Joshua R. , Markopoulos Georgios , Brichacek Matthew , Njardarson Jon T.
Published: March 2011

The core structure (VI) of guttiferone terpenes such as (VII) is prepared via a diacetoxyiodobenzene‐mediated oxidative dearomatization of phenol (II) and a subsequent radical cyclization of the resulting ketal as key steps.
ChemInform Abstract: Phenolic Constituents from the Galls of Pistacia integerrima Stewart
Authors: Ahmad Shamim , Ali Mohammed , Ansari Shahid H.
Published: March 2011

isolation and characterization of pistiphloro‐glucinyl ester (I), pisticiphloroglucinyl ether (II) and pistaciaphenyl ether (III)
ChemInform Abstract: Asymmetric Total Synthesis of (+)‐Fumimycin via 1,2‐Addition to Ketimines.
Authors: Gross Patrick J. , Furche Filipp , Nieger Martin , Braese Stefan
Published: March 2011

The first total synthesis of (+)‐fumimycin, the unnatural enantiomer of the mycotoxin fumimycin, is accomplished.
ChemInform Abstract: Asymmetric Synthesis of the Natural erythro‐(1R,2S)‐8‐O‐4′‐Neolignan Myrislignan.
Authors: Xia Y. , Wang Wei
Published: March 2011

The synthesis of myrislignan (VI) is achieved in twelve steps from vanillin (I) with a total yield of 10% involving two key steps: preparation of the enantiopure threo alcohol (III) of predictable stereochemistry by dihydroxylation, and inversion of the absolute configuration at the C‐8 stereogenic center in (IV) to obtain the title compound with erythro configuration by a Mitsunobu reaction.
ChemInform Abstract: High‐Temperature and High‐Pressure Aqueous Solution Formation, Growth, Crystal Structure, and Magnetic Properties of BiFeO3 Nanocrystals.
Authors: Mi Jian‐Li , Jensen Thomas N. , Christensen Mogens , Tyrsted Christoffer , Joergensen Jens E. , Iversen Bo B.
Published: March 2011

Formation and growth of the title nanocrystals in high‐temperature, high‐pressure aqueous KOH solutions of Fe(NO3)3 and Bi(NO3)3 is monitored by in situ synchrotron powder XRD.
ChemInform Abstract: Condensed Isoquinolines. Part 35. Synthesis and Reactions of 4H‐Thieno[3′,4′:5,6]pyrimido[1,2‐b]isoquinoline‐4,11(5H)‐dione.
Authors: Zadorozhny A. V. , Kovtunenko V. A. , Turov A. V.
Published: March 2011

Compounds (I) are prepared by known methods.
ChemInform Abstract: Cathode Materials for Solid Oxide Fuel Cells: A Review
Authors: Sun Chun‐Wen , Hui Rob , Roller Justin
Published: March 2011

Review: 220 refs.
ChemInform Abstract: Chemistry of the M (M: Fe, Ca, Ba)—Se—H2O Systems at 25 °C
Authors: Nishimura Tadahisa , Hata Ryosuke , Hasegawa Fumihiko
Published: March 2011

Review: 19 refs.
ChemInform Abstract: Access to Highly Fluorinated Silica by Direct F2 Fluorination
Authors: Demourgues Alain , Lataste Emilie , Durand Etienne , Tressaud Alain
Published: March 2011

Review: 71 refs.
ChemInform Abstract: Reactions of Hydrosilanes with Transition Metal Complexes and Characterization of the Products
Authors: Corey Joyce Y.
Published: March 2011

Review: 830 refs.
ChemInform Abstract: Stevioside and Related Compounds — Molecules of Pharmaceutical Promise: A Critical Overview
Authors: Brahmachari Goutam , Mandal Lalan C. , Roy Rajiv , Mondal Sadhan , Brahmachari Arun K.
Published: March 2011

Review: 117 refs.
ChemInform Abstract: Cornerstone Works for Catalytic 1,3‐Dipolar Cycloaddition Reactions
Authors: Kanemasa Shuji
Published: March 2011

Review: 42 refs.
ChemInform Abstract: Guanidine Chemistry
Authors: Ishikawa Tsutomu
Published: March 2011

Review: guanidines as chiral auxiliaries, use for aziridine formation; 31 refs.
ChemInform Abstract: Chemistry of Concerto Molecular Catalysis Based on the Metal/NH Bifunctionality
Authors: Ikariya Takao
Published: March 2011

Review: 110 refs.
ChemInform Abstract: Electroactive Nanotubes from π‐Conjugated Discotic Molecules
Authors: Yamamoto Yohei
Published: March 2011

Review: developments on self‐assembled nanotubes from Gemini‐shaped hexa‐peri‐hexabenzocoronenes; 48 refs.
ChemInform Abstract: A Conjugate Addition—Dipolar Cycloaddition Approach Towards the Synthesis of Various Alkaloids
Authors: Flick Andrew C. , Padwa Albert
Published: March 2011

Review: 177 refs.
ChemInform Abstract: Enzymatic and Chemoenzymatic Approaches Towards Natural and Non‐Natural Alkaloids: Indoles, Isoquinolines, and Others
Authors: Stockigt Joachim , Chen Zhong , Ruppert Martin
Published: March 2011

Review: 157 refs.
ChemInform Abstract: Reactions Within Molecular Single Crystals of Inorganic and Organometallic Compounds: Recent Advances and Implications for Catalysis
Authors: Frech Christian M.
Published: March 2011

Review: 64 refs.
ChemInform Abstract: Key Building Blocks via Enzyme‐Mediated Synthesis
Authors: Fischer Thomas , Pietruszka Joerg
Published: March 2011

Review: 208 refs.
ChemInform Abstract: Metathesis Reactions in Solid‐Phase Organic Synthesis
Authors: Barluenga Sofia , Dakas Pierre‐Yves , Jogireddy Rajamalleswaramma , Valot Gaele , Winssinger Nicolas
Published: March 2011

Review: 88 refs.
ChemInform Abstract: Cascade Metathesis in Natural Product Synthesis
Authors: Porta Marta , Blechert Siegfried
Published: March 2011

Review: 68 refs.
ChemInform Abstract: Metathesis Involving a Relay and Applications in Natural Product Synthesis
Authors: Hoye Thomas R. , Jeon Junha
Published: March 2011

Review: 52 refs.
ChemInform Abstract: Ring‐Closing Alkyne Metathesis in Natural Product Synthesis
Authors: Davies Paul W.
Published: March 2011

Review: 81 refs.
ChemInform Abstract: Phosphorus and Sulfur Heterocycles via Ring‐Closing Metathesis: Application in Natural Product Synthesis
Authors: Thomas Christopher D. , Hanson Paul R.
Published: March 2011

Review: 90 refs.
ChemInform Abstract: Synthesis of Natural Products Containing Medium‐Size Oxygen Heterocycles by Ring‐Closing Alkene Metathesis
Authors: Rainier Jon D.
Published: March 2011

Review: 85 refs.
ChemInform Abstract: Natural Products Containing Medium‐Sized Nitrogen Heterocycles Synthesized by Ring‐Closing Alkene Metathesis
Authors: van den Broek Sebastiaan A. M. W. , Meeuwissen Silvie A. , van Delft Floris L. , Rutjes Floris P. J. T.
Published: March 2011

Review: 100 refs.
ChemInform Abstract: Homogeneous Catalysis Using Lanthanide Amidinates and Guanidinates
Authors: Edelmann Framk T.
Published: March 2011

Review: 72 refs.
ChemInform Abstract: Molecular and Supramolecular Architectures of Organic Semiconductors for Field‐Effect Transistor Devices and Sensors: A Synthetic Chemical Perspective
Authors: Operamolla Alessandra , Farinola Gianluca M.
Published: March 2011

Review: 268 refs.
ChemInform Abstract: Human Protein Atlas of Redox Systems — What Can Be Learnt?
Authors: Dammeyer Pascal , Arner Elias S. J.
Published: March 2011

Review: 89 refs.
ChemInform Abstract: Plant Polyphenols: Chemical Properties, Biological Activities, and Synthesis
Authors: Quideau Stephane , Deffieux Denis , Douat‐Casassus Celine , Pouysegu Laurent
Published: March 2011

Review: 392 refs.
ChemInform Abstract: Targeting DNA Base Pair Mismatch with Artificial Nucleobases. Advances and Perspectives in Triple Helix Strategy
Authors: Malnuit Vincent , Duca Maria , Benhida Rachid
Published: March 2011

Review: 125 refs.
ChemInform Abstract: Activity‐Based Probes: Discovering New Biology and New Drug Targets
Authors: Heal William P. , Dang T. H. Tam , Tate Edward W.
Published: March 2011

Review: 73 refs.
ChemInform Abstract: Orbital Phase Environments and Stereoselectivities
Authors: Ohwada Tomohiko
Published: March 2011

Review: 180 refs.
ChemInform Abstract: An Orbital Phase Theory
Authors: Inagaki Satoshi
Published: March 2011

Review: 146 refs.
ChemInform Abstract: A Mechanistic Spectrum of Chemical Reactions
Authors: Inagaki Satoshi
Published: March 2011

Review: 149 refs.
ChemInform Abstract: Food Analysis and Food Authentication by Peptide Nucleic Acid (PNA)‐Based Technologies
Authors: Sforza Stefano , Corradini Roberto , Tedeschi Tullia , Marchelli Rosangela
Published: March 2011

Review: about 80 refs.
ChemInform Abstract: NMR Methods for Unravelling the Spectra of Complex Mixtures
Authors: Novoa‐Carballal Ramon , Fernandez‐Megia Eduardo , Jimenez Carlos , Riguera Ricardo
Published: March 2011

Review: 161 refs.
ChemInform Abstract: Systems Level Studies of Mammalian Metabolomes: The Roles of Mass Spectrometry and Nuclear Magnetic Resonance Spectroscopy
Authors: Dunn Warwick B. , Broadhurst David I. , Atherton Helen J. , Goodacre Royston , Griffin Julian L.
Published: March 2011

Review: 374 refs.
Wein zwischen Tradition und moderner Technik. Chemie und Genuss
Authors: Otteneder Herbert
Published: March 2011

Die Grundschritte der Weinbereitung sind seit Jahrhunderten gleich geblieben. Geändert haben sich jedoch die technischen Mittel, die entscheidend zur Verbesserung der Weinqualität beigetragen haben. Trotz Reinzuchthefen, Stahltank, Einsatz von Eichenholzspänen, fraktionierter Destillation und einer ganzen Palette von Behandlungsmitteln findet vermehrt auch eine Rückbesinnung auf traditionelle Verfahren statt. An einzelnen Beispielen werden Für und Wider dieser Varianten dargestellt. Das vielfältige und weltweite Angebot der Weine haben auch zur Entwicklung einer ausgefeilten Analytik geführt. Dazu werden u.a. die Möglichkeiten der Authentizitätsprüfung mit Hilfe der Stabilisotopenanalytik aufgezeigt.
Unwiderstehlicher Hefeduft
Authors: Feil Sylvia
Published: March 2011

Fruchtfliegen (Drosopilidae) fliegen normalerweise keine Blüten zum Nektarsammeln an. Doch Aronstab‐Gewächse täuschen sie, um selbst bestäubt zu werden. Die Blüten ahmen den Duft überreifer Früchte nach, von denen sich Fruchtfliegen ernähren und in welche die Weibchen ihre Eier ablegen.
A phase 2 study of tasisulam sodium (LY573636 sodium) as second‐line treatment for patients with unresectable or metastatic melanoma
Authors: Kirkwood John M. , Gonzalez Rene , Reintgen Douglas , Clingan Philip R. , McWilliams Robert R. , de Alwis Dinesh P. , Zimmermann Annamaria , Brown Michael P. , Ilaria Robert L. , Millward Michael J.
Published: March 2011

BACKGROUND:

Tasisulam sodium (hereafter, tasisulam) is a novel anticancer agent that induces apoptosis through the intrinsic pathway and has antiangiogenic activity in preclinical models. Tasisulam demonstrated activity across a broad range of tumors, including melanoma. The primary objective of this phase 2 study was to determine the objective response rate (ORR) in patients who had received 1 previous systemic chemotherapy for unresectable/metastatic melanoma; secondary objectives were to evaluate the clinical response rate (CRR), progression‐free survival (PFS), overall survival (OS), duration of response, safety, and pharmacokinetics.

METHODS:

Tasisulam was administered intravenously on Day 1 of 21‐day cycles according to a lean body weight‐based dosing algorithm targeting a peak plasma concentration (Cmax) of 420 μg/mL.

RESULTS:

In 68 enrolled patients, the median age was 59 years (range, 26‐83 years). No patients had a complete response (CR), 8 patients had a partial response (PR), and 24 patients had stable disease (SD); the ORR (CR + PR) was 11.8%, and the CRR (CR + PR + SD) was 47.1%. The median PFS was 2.6 months, and the median OS was 9.6 months. The predominant treatment‐related grade 3/4 toxicity was thrombocytopenia (20.6% of patients). Tasisulam exhibited a biexponential disposition with a predicted distribution half‐life of 0.3 hours to 2.8 hours and a median terminal elimination half‐life of 10 days (consistent with the turnover of albumin), suggesting that tasisulam is very tightly bound to albumin.

CONCLUSIONS:

Tasisulam administered at a targeted Cmax of 420 μg/mL on Day 1 of 21‐day cycles demonstrated activity and tolerable toxicity as second‐line treatment in malignant melanoma. These results led to a registration trial in metastatic melanoma. Cancer 2011;. © 2011 American Cancer Society.
Impact of BRAF mutation and microsatellite instability on the pattern of metastatic spread and prognosis in metastatic colorectal cancer
Authors: Tran Ben , Kopetz Scott , Tie Jeanne , Gibbs Peter , Jiang Zhi‐Qin , Lieu Christopher H. , Agarwal Atin , Maru Dipen M. , Sieber Oliver , Desai Jayesh
Published: March 2011

BACKGROUND:

It is hypothesized that BRAF mutant cancers represent a discrete subset of metastatic colorectal cancer (CRC) defined by poorer survival. This study investigates whether BRAF mutant CRC is further defined by a distinct pattern of metastatic spread and explores the impact of BRAF mutation and microsatellite instability (MSI) on prognosis in metastatic CRC.

METHODS:

By using prospective clinical data and molecular analyses from 2 major centers (Royal Melbourne Hospital and The University of Texas MD Anderson Cancer Center), patients with known BRAF mutation status were analyzed for clinical characteristics, survival, and metastatic sites.

RESULTS:

The authors identified 524 metastatic CRC patients where BRAF mutation status was known; 57 (11%) were BRAF mutant tumors. BRAF mutant tumors were significantly associated with right‐sided primary tumor, MSI, and poorer survival (median, 10.4 months vs 34.7 months, P < .001). A distinct pattern of metastatic spread was observed in BRAF mutant tumors, namely higher rates of peritoneal metastases (46% vs 24%, P = .001), distant lymph node metastases (53% vs 38%, P = .008), and lower rates of lung metastases (35% vs 49%, P = .049). In additional survival analyses, MSI tumors had significantly poorer survival compared with microsatellite stable tumors (22.1 months vs 11.1 months, P = .017), but this difference was not evident in the BRAF mutant population.

CONCLUSIONS:

The pattern of metastatic spread observed in this study further defines BRAF mutant CRC as a discrete disease subset. The authors demonstrated that, unlikely early stage disease, MSI is associated with poorer survival in metastatic CRC, although this is driven by its association with BRAF mutation. Cancer 2011;. © 2011 American Cancer Society.
Nonmyeloablative allogeneic stem cell transplantation in relapsed/refractory chronic lymphocytic leukemia
Authors: Khouri Issa F. , Bassett Roland , Poindexter Nancy , O'Brien Susan , Bueso‐Ramos Carlos E. , Hsu Yvonne , Ferrajoli Alessandra , Keating Michael J. , Champlin Richard , Fernandez‐Vina Marcelo
Published: March 2011

BACKGROUND:

The role of nonmyeloablative allogeneic stem cell transplantation (NST) in the treatment of chronic lymphocytic leukemia (CLL) is not well established. The authors report on long‐term experience with NST in relapsed/refractory CLL and define prognostic factors associated with outcome.

METHODS:

The authors reviewed the outcome of 86 patients with relapsed/relapsed CLL enrolled in sequential NST protocols.

RESULTS:

The median patient age was 58 years. Patients were heavily pretreated before transplantation, and 43 required immunomanipulation after NST for persistent or recurrent disease. Immunomanipulation included withdrawal of immunosuppression, rituximab, and step‐wise donor lymphocyte infusions. Of 43 patients receiving immunomanipulation, 20 (47%) experienced a complete remission. Patients with human leukocyte antigen (HLA) genotype A1+/A2−/B44− were more likely to experience a complete remission (P = .0009), with rates of 9%, 36%, 50%, and 91%, respectively, for 0, 1, 2, and 3 of these HLA factors. This resulted in significant improvement in progression‐free‐survival rates of 68.2% at 5 years for patients with all 3 HLA factors. Overall, the estimated 5‐year survival rate was 51%. In a multivariate model, a CD4 count of <100/mm3 and a below normal serum immunoglobulin G level at study entry were associated with a short survival duration (P < .0001).

CONCLUSIONS:

These results confirm the potential cure of relapsed/refractory CLL with NST and provide the first evidence that immunoglobulin G and CD4 levels are predictive of overall survival after NST in CLL and that human leukocyte antigen alleles predict response to immunomanipulation. Cancer 2011;. © 2011 American Cancer Society.
Increasing accrual in cancer clinical trials with a focus on minority enrollment
Authors: Vicini Frank , Nancarrow‐Tull Joyce , Shah Chirag , Chmielewski Gary , Fakhouri Monty , Sitarek Stacey A. , Feczko Claire T. , Brzozowski Carol , Felten David L.
Published: March 2011

BACKGROUND:

The authors reviewed changes in accrual to cancer clinical trials over the last 2 decades at their institution with a focus on minority participation after the implementation of a community clinical oncology program (CCOP) and an aggressive, education‐orientated minority outreach program (MOP).

METHODS:

Data on patient enrollment in clinical trials for the years 1988 to 2010 was obtained from the William Beaumont Hospital (WBH) Cancer Clinical Trials Office. The type and number of cancers diagnosed and treated during the same period were obtained from the WBH tumor registry data. The MOP was initiated in the fall of 2003 with a focus on culture‐specific cancer education.

RESULTS:

With the development of the CCOP, clinical trials accrual increased significantly by 10‐fold (P = .001). The primary service area for the CCOP consistently averaged an 85% to 90% Caucasian population. During the same period, the minority population for the service area remained stable between 8.8% and 10% and did not change significantly. From 1999 to 2004, the WBH tumor registry data demonstrated that minorities represented 8.6% of cancers registered, whereas the average yearly minority enrollment from 2002 to 2004 was 5.4%. After initiation of the MOP, minority accrual doubled to 11% by 2010 with stable minority demographics.

CONCLUSIONS:

The current findings support the importance of a CCOP in supporting the accrual of patients to national clinical trials and increasing access to state‐of‐the art research. These data also strongly support focusing additional energy and educational efforts on targeting minority representation in clinical trials. Cancer 2011;. © 2011 American Cancer Society.
Phase 1 study of arsenic trioxide, high‐dose cytarabine, and idarubicin to down‐regulate constitutive signal transducer and activator of transcription 3 activity in patients aged <60 years with acute myeloid leukemia
Authors: Wetzler Meir , Andrews Chris , Ford Laurie A. , Tighe Sheila , Barcos Maurice , Sait Sheila N. J. , Block AnneMarie W. , Nowak Norma J. , Baer Maria R. , Wang Eunice S. , Baumann Heinz
Published: March 2011

BACKGROUND:

Constitutive activation of signal transducer and activator of transcription‐3 (STAT3) was detected in blasts from approximately 50% of patients with acute myeloid leukemia (AML) and was correlated with an adverse outcome. In vitro treatment of AML blasts with arsenic trioxide (ATO) down‐regulated STAT3 activity within 6 hours associated with a reduced viability within 48 hours.

METHODS:

A phase 1 clinical trial to evaluate the biologically effective dose and/or the maximally tolerated dose (MTD) of ATO in vivo in conjunction with high‐dose cytarabine (Hidac) and idarubicin (Ida) in patients with AML aged <60 years was conducted. Data were compared with 117 historic AML patients who had received treatment with Hidac/Ida.

RESULTS:

In total, 61 patients were enrolled onto 11 different dose levels (from 0.01 to 0.65 mg/kg ideal body weight). The MTD was 0.5 mg/kg. Compared with historic controls, patients who received ATO/Hidac/Ida, although they had similar pretreatment characteristics, had better overall survival (P = .039).

CONCLUSIONS:

ATO priming may have improved the outcome of patients aged <60 years with AML who received Hidac/Ida. The current data suggested that ATO may enhance the effect of chemotherapy. The authors concluded that further studies of this novel combination are warranted. Cancer 2011;. © 2011 American Cancer Society.