bluuebunny/crossref_metadata_2025_split huggingface dataset:
ChemInform Abstract: Growth and Characterization of Tetragonal Structure Modification of β‐Gd2Si2O7:Ce.
Authors: Baumer V. , Gerasymov I. , Sidletskiy O. , Voloshina O. , Neicheva S. 
Published: November 2012

Abstractβ‐Gd2Si2O7 doped with 5 at.% Ce is prepared by solid state reaction of a near‐peritectic mixture of Gd2O3, SiO2, and CeO2 (1700 °C).
ChemInform Abstract: Two Highly Proton‐Conductive Molecular Hybrids Based on Ionized Water Clusters and Poly‐Keggin‐Anion Chains.
Authors: Wei Mei‐Lin , Zhuang Peng‐Fei , Miao Qiu‐Xiang , Wang Yan 
Published: November 2012

AbstractAs revealed by single crystal XRD the molecular hybrid complexes (IIIa, b) crystallize in the orthorhombic space group Pnnm with Z = 2 and exhibit the same three‐dimensional hydrogen‐bonded networks with large one‐dimensional channels filled with [PMo12O40]3‐ anions which are self‐assembled into poly‐Keggin‐anion chains.
ChemInform Abstract: Synthesis, Crystal Structure, and Physical Properties of the New Chain Alkalioxocuprate K3Cu2O4.
Authors: Duris Katarina , Kremer Reinhard K. , Jansen Martin 
Published: November 2012

AbstractBlack needle shaped single crystals of the title compound are prepared by reaction of a stoichiometric mixture of KN3, KNO3, and CuO (closed steel container, controlled heating, 923 K, 50 h).
ChemInform Abstract: Iron(II)‐Catalyzed Amidation of Aldehydes with Iminoiodinanes at Room Temperature and under Microwave‐Assisted Conditions
Authors: Ton Thi My Uyen , Tejo Ciputra , Tania Stefani , Chang Joyce Wei Wei , Chan Philip Wai Hong 
Published: November 2012

Abstractas an efficient and straightforward access to a wide range of amides
ChemInform Abstract: Enantioselective Iridium‐Catalyzed Allylic Substitutions with Hydroxamic Acid Derivatives as N‐Nucleophiles.
Authors: Gaertner Martin , Jaekel Mascha , Achatz Manuel , Sonnenschein Christoph , Tverskoy Olena , Helmchen Guenter 
Published: November 2012

AbstractDifferent protocols are developed for the regio‐ and enantioselective allylic aminations of various hydroxamic acid derivatives.
ChemInform Abstract: Simple and Efficient Synthesis of N‐Nitroethylenediamine Derivatives.
Authors: Kvapil Lubomir , Simacek Adam , Grepl Martin , Gucky Tomas , Pospisil Tomas , Hradil Pavel 
Published: November 2012

Abstract1‐Nitroimidazolidin‐2‐one (I) undergoes ring‐opening with nucleophiles to yield products of type (III).
ChemInform Abstract: N‐Allyl‐N‐sulfonyl Ynamides as Synthetic Precursors to Amidines and Vinylogous Amidines. An Unexpected N‐to‐C 1,3‐Sulfonyl Shift in Nitrile Synthesis.
Authors: DeKorver Kyle A. , Johnson Whitney L. , Zhang Yu , Hsung Richard P. , Dai Huifang , Deng Jun , Lohse Andrew G. , Zhang Yan‐Shi 
Published: November 2012

AbstractThe Pd‐catalyzed or thermally‐induced treatment of ynamides of type (I) with amines allows convenient access to amidines.
ChemInform Abstract: Oxidative, Photoactivated TiO2 Nanoparticles in the Catalytic Acetylation of Primary Alcohols.
Authors: Chen Chien‐Tien , Kao Jun‐Qi , Liu Cheng‐Yuan , Jiang Ling‐Yu 
Published: November 2012

AbstractThe size of the nanoparticles and their preactivation with H2O2 are crucial.
ChemInform Abstract: Abnormal Ito—Saegusa Oxidation of TIPS Enol Ether Assisted by a Hydroxy Group on a Side Chain.
Authors: Hiraoka Shiharu , Harada Shinji , Nishida Atsushi 
Published: November 2012

AbstractAlthough Ito‐Saegusa oxidation gives defined α,β‐unsaturated ketones from silyl enol ether of ketones, controlled by the position of the sp2 carbon of the silyl enol ether, the formation of a regioisomeric product that is oxidized abnormally is observed.
ChemInform Abstract: Highly Enantioselective Nitroaldol Reactions Catalyzed by Copper(II) Complexes Derived from Substituted 2‐(Pyridin‐2‐yl)imidazolidin‐4‐one Ligands.
Authors: Panov Illia , Drabina Pavel , Padelkova Zdenka , Stimunek Petr , Sedlak Milos 
Published: November 2012

AbstractSome chiral pyridinylimidazolidinones of type (I) are prepared and tested.
ChemInform Abstract: Synthesis of Nipagin Esters Using Acidic Functional Ionic Liquids as Catalysts.
Authors: Wang Guohua , Li Lu , Xie Congxia , Yu Shitao , Liu Fusheng , Ye Xiaoling 
Published: November 2012

AbstractSeveral Broensted acidic functional ionic liquids are synthesized and tested as dual solvent‐catalysts for the synthesis of nipagin esters (III).
ChemInform Abstract: Asymmetric Mannich Reactions Catalyzed by Cinchona Alkaloid Thiourea: Enantioselective One‐Pot Synthesis of Novel β‐Amino Ester Derivatives.
Authors: Bai Song , Liang Xueping , Song Baoan , Bhadury Pinaki S. , Hu Deyu , Yang Song 
Published: November 2012

AbstractA variety of aromatic and aliphatic aldehydes is applied and enantioselectivities up to 99% e.e.
ChemInform Abstract: Nickel‐Catalyzed Cycloadditions of Benzoxazinones with Alkynes: Synthesis of Quinolines and Quinolones.
Authors: Maizuru Nobuyoshi , Inami Tasuku , Kurahashi Takuya , Matsubara Seijiro 
Published: November 2012

AbstractThe reaction outcome is determined by the C‐2 substituent of the benzoxazinone.
ChemInform Abstract: Copper‐Catalyzed Cascade Synthesis of Alkyl 6‐Aminobenzimidazo[2,1‐a]isoquinoline‐5‐carboxylates.
Authors: Lu Juyou , Fu Hua 
Published: November 2012

AbstractTreatment of benzimidazoles of type (I) with cyanoacetates allows a new and efficient access to title compounds like (III) which are of biological interest.
ChemInform Abstract: Synthesis, Chemical Properties, and Antimicrobial Activity of 2‐ and 2,3‐Substituted [(Tetrahydro‐2,4‐dioxopyrimidin‐1(2H)‐yl)phenoxy] naphthalene‐1,4‐diones.
Authors: Voskiene Ausra , Sapijanskaite Birute , Mickevicius Vytautas , Kantminiene Kristina , Stasevych Maryna , Komarovska‐Porokhnyavets Olena , Musyanovych Rostyslav , Novikov Volodymyr 
Published: November 2012

AbstractMono‐ and disubstituted title naphthalene‐1,4‐diones are synthesized and tested for their stability in alkaline and acidic media.
ChemInform Abstract: A Novel Approach for the One‐Pot Synthesis of Linear and Angular Fused Quinazolinones.
Authors: Maity Arindam , Mondal Shyamal , Paira Rupankar , Hazra Abhijit , Naskar Subhendu , Sahu Krishnendu B. , Saha Pritam , Banerjee Sukdeb , Mondal Nirup B. 
Published: November 2012

AbstractA two‐step one‐pot protocol is developed for the synthesis of a series of title compounds including different benzofused analogues.
ChemInform Abstract: Synthetic Utility of Bifunctional Thiophene Derivatives and Antimicrobial Evaluation of the Newly Synthesized Agents.
Authors: Abu‐Hashem Ameen A. , Abu‐Zied Khadiga M. , El‐Shehry Mohamed F. 
Published: November 2012

AbstractRapid and effective procedures for the synthesis of various thiophene and thienopyrimidine derivatives starting from 2‐aminothiophenecarboxylate (I) are developed.
ChemInform Abstract: A Simple Synthesis of 4‐Substituted 2,3‐Benzoxazinones from C‐2 Arylated 1,3‐Indanediones.
Authors: Das Suven , Koley Pradyot , Pramanik Animesh 
Published: November 2012

AbstractThe title transformation constitutes an acid‐catalyzed rearrangement followed by condensation with hydroxylamine.
ChemInform Abstract: Et2MeN·HI‐Catalyzed Reaction of Arylboronic Acids with 2‐Acyl‐2,3‐dihydro‐4H‐pyrans Leading to 2‐Aryltetrahydrocyclopenta[1,3,2]dioxaboroles.
Authors: Fukuyama Takahide , Okamura Takahiro , Ryu Ilhyong 
Published: November 2012

AbstractThe novel ring contraction involves ring‐opening to give intermediate 2‐hydroxy‐1,6‐diketones such as (IV) which can be isolated in the absence of boronic acid.
ChemInform Abstract: A Novel Fumed Silica‐Supported Nitrogenous Platinum Complex as a Highly Efficient Catalyst for the Hydrosilylation of Olefins with Triethoxysilane.
Authors: Li Ji , Yang Chunhui , Zhang Lei , Ma Tianlong 
Published: November 2012

AbstractA new catalyst is prepared from H2PtCl6 and fumed aminopropyl silica and successfully applied in the hydrosilylation of terminal olefins.
ChemInform Abstract: Tabulvelutin A, the First 19‐Nor Limonoid with Unprecedented Ring System from Chukrasia tabularis var. velutina.
Authors: Yin Jun‐Lin , Di Ying‐Tong , Fang Xin , Liu En‐De , Liu Hai‐Yang , He Hong‐Ping , Li Shun‐Lin , Li Shi‐Fei , Hao Xiao‐Jiang 
Published: November 2012

AbstractTitle compound (I) together with a bio‐synthetically related limonoid tabulvelutin B (II) show no significant insecticidal activity against Flutella xylostella and Heliothis virescens.
ChemInform Abstract: A New Efficient Synthetic Method for 3‐Iodothyronamine Involving Sonication and Its Potent Hypothermic Efficacy.
Authors: Kim Joong‐Gon , Song Young‐Kyu , Jo Ye‐Hyun , Yu Mi‐Ran , Ju Hyunwoo , Choi Inho , Chung Chan‐Moon 
Published: November 2012

AbstractThe introduced synthesis has the advantages of reduced synthetic steps and significantly enhanced overall yield compared to the conventional method.
ChemInform Abstract: Enhanced Superconductivity of SmFeAsO Co‐Doped by Scandium and Fluorine to Increase Chemical Inner Pressure.
Authors: Chen Haijie , Zheng Ming , Fang Aihua , Yang Jianhua , Huang Fuqiang , Xie Xiaoming , Jiang Mianheng 
Published: November 2012

AbstractThe compounds Sm1‐x/3Scx/3FeAsO1‐xFx (x = 0.09—0.27) are synthesized by mechanical alloying of SmAs, Fe2As, FeO, SmOF, and Sc2O3 followed by sintering at 1223 K for 2 h.
ChemInform Abstract: High Magnetic Ordering Temperature in the Perovskites Sr4‐xLaxFe3ReO12 (x = 0.0, 1.0, 2.0).
Authors: Greenblatt M. , et al. et al. 
Published: November 2012

AbstractThe title compounds are prepared by the citrate—nitrate method and characterized by powder XRD and neutron diffraction, TEM, SEM, XANES, Moessbauer spectroscopy, and magnetic measurements.
ChemInform Abstract: Synthesis and Magnetic Properties of the High‐Pressure Scheelite‐Type GdCrO4 Polymorph.
Authors: Dos santos‐Garcia A. J. , Climent‐Pascual E. , Gallardo‐Amores J. M. , Rabie M. G. , Doi Y. , Romero de Paz J. , Beuneu B. , Saez‐Puche R. 
Published: November 2012

AbstractThe title compound is obtained from zircon‐type GdCrO4 (Pt crucible, 4 GPa, 803 K, 30 min).
ChemInform Abstract: Inorganic Crown Ethers: Sulfate‐Based Preyssler Polyoxometalates.
Authors: Zhang Zhi‐Ming , Yao Shuang , Li Yang‐Guang , Han Xin‐Bao , Su Zhong‐Min , Wang Zhi‐Shu , Wang En‐Bo 
Published: November 2012

AbstractThe new Preyssler polyoxoanion [S5W30O110]10‐ incorporates a position‐specific K+ or Na+ ion in its geometrical center.
ChemInform Abstract: Crystal Structure, Electrical Resistivity, and X‐Ray Photoelectron Spectroscopy of BaAg2As2.
Authors: Stoyko Stanislav S. , Blanchard Peter E. R. , Mar Arthur 
Published: November 2012

AbstractThe title compound is synthesized by reaction of a stoichiometric mixture of the elements (alumina crucible, 850 °C for 2 d and 800 °C for 7 d).
ChemInform Abstract: Reactions of 6‐(Tri‐ and 6‐(Difluoromethyl))comanic Acids and Their Ethyl Esters with Aniline and Its 2‐Substituted Derivatives.
Authors: Obydennov Dmitrii L. , Usachev Boris I. 
Published: November 2012

AbstractDerivative (VI) can be easily converted to (V) when the crude product mixture is heated in DMSO at 120 °C.
ChemInform Abstract: Cu(OTf)2‐Catalyzed Ritter Reaction: Efficient Synthesis of Amides from Nitriles and Halohydrocarbons in Water.
Authors: Qu Gui‐Rong , Song Yan‐Wei , Niu Hong‐Ying , Guo Hai‐Ming , Fossey John S. 
Published: November 2012

AbstractA wide range of amides is smoothly synthesized by Ritter reaction of benzyl, tert‐butyl, sec‐alkyl and primary alkyl halides with various nitriles.
ChemInform Abstract: Ruthenium‐Catalyzed One‐Pot Synthesis of S‐Allyl and Cinnamyl Dithiocarbamates Using Allyl and Cinnamyl Acetates in Water.
Authors: Ahammed Sabir , Saha Amit , Ranu Brindaban C. 
Published: November 2012

AbstractA wide range of new cinnamyl‐ and allyl dithiocarbamates is prepared by the new reaction of the appropriate cinnamyl‐ and allyl acetate, carbon disulfide an an amine in the presence of Ru(acac)3 in water.
ChemInform Abstract: Ruthenium(II) Pincer Complexes with Oxazoline Arms for Efficient Transfer Hydrogenation Reactions.
Authors: Chen Tao , He Li‐Peng , Gong Dirong , Yang Limin , Miao Xiaohe , Eppinger Joerg , Huang Kuo‐Wei 
Published: November 2012

AbstractThe design of novel pincer ligands is described.
ChemInform Abstract: Direct Catalytic Asymmetric Synthesis of Highly Functionalized (2‐Ethynylphenyl)alcohols via Barbas—List Aldol Reaction: Scope and Synthetic Applications.
Authors: Ramachary Dhevalapally B. , Mondal Rumpa , Madhavachary R. 
Published: November 2012

AbstractThe present method furnishes valuable building blocks for preparation of medicinically interesting compounds and ligands for asymmetric synthesis.
ChemInform Abstract: Convenient Synthesis and Characterization of Molecules Containing Multiple β‐Keto Ester Units.
Authors: Belmar Julio , Ortiz Leandro , Ramirez Denis , Fuentes Fabiola , Para Maria , Jimenez Veronica A. , Jimenez Claudio A. 
Published: November 2012

AbstractCompounds containing 2 or 3 β‐keto ester units are obtained via reaction of acid chlorides with ethyl cyanoacetate in the presence of barium oxide.
ChemInform Abstract: Palladium‐Catalyzed Suzuki—Miyaura Coupling with Aryl and Heteroaryl Bromides Using N,N,N′,N′‐Tetra(diphenylphosphinomethyl)‐1,2‐ethylenediamines.
Authors: Wang Kun , Yi Tao , Yu Xiaojun , Zheng Xueli , Fu Haiyan , Chen Hua , Li Ruixiang 
Published: November 2012

AbstractA wide range of biaryl is synthesized using a new catalyst containing PdCl2 and a tetraphosphine ligand.
ChemInform Abstract: Synthesis of Stilbene Analogues by One‐Pot Oxidation‐Wittig and Oxidation‐Wittig—Heck Reaction.
Authors: Saiyed Akeel S. , Patel Krupa N. , Kamath Bola V. , Bedekar Ashutosh V. 
Published: November 2012

AbstractSynthesis of symmetrical and unsymmetrical stilbene derivatives (II), (VII), and (X) is achieved by a combination of one‐pot steps of Kornblum type oxidation of benzyl halide (I), its simultaneous in situ formation of phosphonium salt, and subsequent Wittig reaction.
ChemInform Abstract: Enantioselective Synthesis of trans‐Dihydrobenzofurans via Primary Amine‐Thiourea Organocatalyzed Intramolecular Michael Addition.
Authors: Lu Aidang , Hu Keling , Wang Youming , Song Haibin , Zhou Zhenghong , Fang Jianxin , Tang Chuchi 
Published: November 2012

AbstractAn efficient and highly enantioselective method to prepare trans‐dihydrobenzofurans and trans‐dihydronaphthofurans is reported.
ChemInform Abstract: Phenyl α‐Bromovinyl Sulfone in Cycloadditions with Azomethine Ylides: An Unexpected Facile Aromatization of the Cycloadducts into Pyrroles.
Authors: Kudryavtsev Konstantin V. , Ivantcova Polina M. , Churakov Andrei V. , Vasin Victor A. 
Published: November 2012

Abstract1,3‐Dipolar cycloaddition of azomethine ylides with vinyl sulfone (I) proceeds in the presence of catalytic amounts of silver acetate and DBU to give pyrrolidine cycloadducts (IV) and (V) regioselectively.
ChemInform Abstract: Synthesis of 3‐Diazopyrrolidin‐2‐ones.
Authors: Galina Yu. R. , Lobov A. N. , Sultanova R. M. , Dokichev V. A. , Tomilov Yu. V. 
Published: November 2012

AbstractTitle compounds (II) and (VI) are synthesized by reaction of amines (I) or (V), resp., with isopentyl nitrite.
ChemInform Abstract: Assisted Tandem Catalytic RCM‐Aromatization in the Synthesis of Pyrroles and Furans.
Authors: Schmidt Bernd , Krehl Stefan , Jablowski Eric 
Published: November 2012

AbstractThe present method relies on the conversion of the metathesis catalyst into a dehydrogenation catalyst by treatment with aqueous tBuOOH in situ.
ChemInform Abstract: Automated Multistep Continuous Flow Synthesis of 2‐(1H‐Indol‐3‐yl)thiazole Derivatives.
Authors: Pagano Nicholas , Heil Marintha L. , Cosford Nicholas D. P. 
Published: November 2012

AbstractA consecutive heterocycle formation is developed from thioamide (I), bromoketones (II) and arylhydrazones (III) using an automated continuous flow process to give indolylthiazoles in moderate yields.
ChemInform Abstract: Secondary Amine Catalyzed Asymmetric Michael Addition of N‐tert‐Butoxycarbonyl‐Protected Oxindoles to Maleimides.
Authors: Yang Xuena , Wang Chuan , Ni Qijian , Enders Dieter 
Published: November 2012

AbstractThe reaction proceeds through a Broenstedt base activation mode with DPS as the optimal catalyst.
ChemInform Abstract: Nucleophilic Addition of Grignard Reagents to 3—Acylindoles: Stereoselective Synthesis of Highly Substituted Indoline Scaffolds.
Authors: Wang Lu , Shao Yushang , Liu Yuanhong 
Published: November 2012

AbstractThe reaction results in efficient formation of either trans‐ or cis‐substituted indolines depending on the quenching procedure used.
ChemInform Abstract: Synthesis and Biological Evaluation of Phenyl Substituted 1H‐1,2,4‐Triazoles as Non‐Steroidal Inhibitors of 17β‐Hydroxysteroid Dehydrogenase Type 2.
Authors: Al‐Soud Yaseen A. , Marchais‐Oberwinkler Sandrine , Frotscher Martin , Hartmann Rolf W. 
Published: November 2012

AbstractTitle compounds, e.g. (IV) and (X), are synthesized and evaluated as 17βHSD2 inhibitors.
ChemInform Abstract: Synthesis of Enantiopure Dehydropiperidinones from α‐Amino Acids and Alkynes via Azetidin‐3‐ones.
Authors: Ishida Naoki , Yuhki Tatsuya , Murakami Masahiro 
Published: November 2012

AbstractThe Ni‐catalyzed treatment of the azetidinones allows a new access to optically active dehydropiperidinones.
ChemInform Abstract: Base‐Promoted Heterocyclization of Fluorinated Alkynylphosphonates with Select ortho‐Aminobenzonitriles.
Authors: Duda Blazej , Tverdomed Sergey N. , Ionin Boris I. , Roeschenthaler Gerd‐Volker 
Published: November 2012

AbstractThe process affords mainly or exclusively highly substituted 4‐aminoquinoline structures.
ChemInform Abstract: An Alternative Strategy to the Pictet—Spengler Method for Tetrahydroisoquinoline Synthesis: A Feasibility Study.
Authors: Henderson Laura , Knight David W. , Williams Andrew C. 
Published: November 2012

AbstractAcid‐catalyzed cyclizations of 2‐aminoethyl styrene derivatives (I), (III) and (V) give the corresponding tetrahydroisoquinolines (II), (IV), and (VI) by an intramolecular hydroamination reaction, which represents an alternative and potentially more flexible strategy to the Pictet‐Spengler cyclization.
ChemInform Abstract: Intramolecular C—C Coupling of 2,6‐Disubstituted‐1‐bromoaryls for Dihydrophenanthridines.
Authors: Singh Vijay P. , Singh Puspendra , Singh Harkesh B. , Butcher Ray J. 
Published: November 2012

AbstractAn unexpected intramolecular coupling of imines (I) and (III) under conditions A) produces the title compounds as major or sole products.
ChemInform Abstract: An Efficient Synthesis of 4‐Naphthylpyrimidin‐2‐amine Derivatives under Solvent‐Free Conditions.
Authors: Rong Liangce , Ji Honglou , Xia Sheng , Yin Shan , Shi Yanhui , Tu Shujiang 
Published: November 2012

AbstractThe methodology has the advantages of operational simplicity, high efficiency, low costs and mild reaction conditions.
ChemInform Abstract: Synthesis of New Aza Macrocyclic Diamides 2,2′‐Diaminodiphenyl Sulfide Using Crab‐Like Method.
Authors: Shockravi Abbas , Kamali Mahmood 
Published: November 2012

AbstractReaction of bis‐α‐chloroacetamidediphenylsulfide (III) as crab‐like condensing reagent with different diamines leads to corresponding aza‐thia and oxa macrocycles such as (V), (VII).
ChemInform Abstract: A Sensitive Colorimetric and Ratiometric Fluorescent Probe for Mercury Species in Aqueous Solution and Living Cells.
Authors: Jiang Jie , Liu Wei , Cheng Ju , Yang Lizi , Jiang Huie , Bai Decheng , Liu Weisheng 
Published: November 2012

AbstractA new fluorescent probe for inorganic and organic mercury species based on mercury triggered cleavage reaction is developed.
ChemInform Abstract: Design, Synthesis and Biological Evaluation of Novel Acrylamide Analogues as Inhibitors of BCR—ABL Kinase.
Authors: Hu Wenxiang , et al. et al. 
Published: November 2012

AbstractThe acrylamide analogues, related to Imatinib and Nilotinib, are synthesized by application of the principle of nonclassical electronic isostere.
Separation Technologies 2030 – Are 100 Years of Chromatography Enough?
Authors: Ditz Reinhard 
Published: November 2012

AbstractChromatography has provided significant contributions to the fields of molecule characterization as well as purification over the last century, thereby being quite unique in its flexibility and scaleability. The development of biotherapeutics would have been impossible without chromatography‐based purification strategies. Future areas for exploitation are the combination with other separation concepts together with model‐based approaches for materials and process design.
Directed Modulation of Protein Kinase C Isozyme Selectivity with Bisubstrate‐Based Inhibitors
Authors: van Wandelen Loek T. M. , van Ameijde Jeroen , Mady Ahmed S. A. , Wammes Angelique E. M. , Bode Alois , Poot Alex J. , Ruijtenbeek Rob , Liskamp Rob M. J. 
Published: November 2012

AbstractKinases present an attractive target for drug development, since they are involved in vital cellular processes and are implicated in a variety of diseases, such as cancer and diabetes. However, obtaining selectivity for a specific kinase over others is difficult since many current kinase inhibitors exclusively target the highly conserved kinase ATP binding domain. Previously, a microarray‐based strategy to discover so‐called bisubstrate‐based inhibitors that target the more specific peptide binding groove in addition to the ATP binding site was described. One attractive feature of this strategy is the opportunity to tune the selectivity of these inhibitors by systematically varying components. In an extension to this previous work, this study explores the potential of this guided selectivity modulation, leading to a series of inhibitors with different selectivity profiles against highly homologous protein kinase C (PKC) isozymes. Of the inhibitors studied, most exhibited improved potency and selectivity compared with their constituent parts. Furthermore, the selectivity was found to be tunable either through modification of the pseudosubstrate peptide (peptide binding groove) or the ATP‐competitive part (ATP binding site). In a number of cases, the selectivity of the construct could be predicted from the initial peptide substrate profiling experiment. Since this strategy is applicable to all kinase sets, it could be used to rapidly develop uniquely selective inhibitors.
Identification of Small Molecules that Interfere with H1N1 Influenza A Viral Replication
Authors: Bottini Angel , De Surya K. , Baaten Bas J. G. , Wu Bainan , Barile Elisa , Soonthornvacharin Stephen , Stebbins John L. , Bradley Linda M. , Chanda Sumit K. , Pellecchia Maurizio 
Published: November 2012

AbstractSuccessful replication of the influenza A virus requires both viral proteins and host cellular factors. In this study we used a cellular assay to screen for small molecules capable of interfering with any of such necessary viral or cellular components. We used an established reporter assay to assess influenza viral replication by monitoring the activity of co‐expressed luciferase. We screened a diverse chemical compound library, resulting in the identification of compound 7, which inhibits a novel yet elusive target. Quantitative real‐time PCR studies confirmed the dose‐dependent inhibitory activity of compound 7 in a viral replication assay. Furthermore, we showed that compound 7 is effective in rescuing high‐dose influenza infection in an in vivo mouse model. As oseltamivir‐resistant influenza strains emerge, compound 7 could be further investigated as a new and potentially suitable scaffold for the development of anti‐influenza agents that act on novel targets.