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文章名     作者     期刊名     摘要     卷     期         如果没有找到您所需要的文献，请点击 ——此处申请     共23条记录   Phosphoramidate ProTides of 2 '-C-Methylguanosine as Highly Potent Inhibitors of Hepatitis C Virus. Study of Their in Vitro and in Vivo Properties [作者：MCGUIGAN CHRISTOPHER; GILLES ARNAUD; MADELA KAROLINA; ALJARAH MOHAMED; HOLL SABRINA; JONES SARAH; VERNACHIO JOHN; HUTCHINS JEFF; AMES BRENDA; BRYANT K DAWN; GOROVITS ELENA; GANGULY BABITA; HUNLEY DAMOUND; HALL ANDREA; KOLYKHALOV ALEXANDER; LIU YULE; MUHAMMAD JERRY; RAJA NICHOLAS; WALTERS ROBIN; WANG JIN; CHAMBERLAIN STANLEY; HENSON GEOFFREY,期刊：Journal of Medicinal Chemistry, 页码：4949-4957 , 文章类型： Article，,卷期：2010年53-13] Hepatitis C virus infection constitutes a serious health problem in need of more effective therapies. Nucleoside analogues with improved exposure, efficacy, and selectivity are recognized as likely key components of futu... Discovery and Optimization of Boronic Acid Based Inhibitors of Autotaxin [作者：ALBERS HARALD M H G; VAN MEETEREN LAURENS A; EGAN DAVID A; VAN TILBURG ERICA W; MOOLENAAR WOUTER H; OVAA HUIB,期刊：Journal of Medicinal Chemistry, 页码：4958-4967 , 文章类型： Article，,卷期：2010年53-13] Autotaxin (ATX) is an extracellular enzyme that hydrolyzes lysophosphatidylcholine (LPC) to produce the lipid mediator lysophosphatidic acid (LPA). The ATX LPA signaling axis has been implicated in diverse physiological ... Severe Acute Respiratory Syndrome Coronavirus Papain-like Novel Protease Inhibitors: Design, Synthesis, Protein-Ligand X-ray Structure and Biological Evaluation [作者：GHOSH ARUN K; TAKAYAMA JUN; RAO KALAPALA VENKATESWARA; RATIA KIIRA; CHAUDHURI RIMA; MULHEARN DEBBIE C; LEE HYUN; NICHOLS DANIEL B; BALIJI SURENDRANATH; BAKER SUSAN C; JOHNSON MICHAEL E; MESECAR ANDREW D,期刊：Journal of Medicinal Chemistry, 页码：4968-4979 , 文章类型： Article，,卷期：2010年53-13] The design, synthesis, X-ray crystal structure, molecular modeling, and biological evaluation of a series of new generation SARS-CoV PLpro inhibitors are described. A new lead compound 3 (6577871) was identified via high... Fast-Forwarding Hit to Lead: Aurora and Epidermal Growth Factor Receptor Kinase Inhibitor Lead Identification [作者：COUMAR MOHANE SELVARAJ; CHU CHANGYING; LIN CHENGWEI; SHIAO HUIYI; HO YUNLUNG; REDDY RANDHEER; LIN WENHSING; CHEN CHUNHWA; PENG YIHUI; LEOU JIUNSHYANG; LIEN TZUWEN; HUANG CHINTING; FANG MINGYU; WU SZUHUEI; WU JIANSUNG; CHITTIMALLA SANTHOSH KUMAR; SONG JENSHIN; HSU JOHN T A; WU SUYING; LIAO CHUNCHEN; CHAO YUSHENG; HSIEH HSINGPANG,期刊：Journal of Medicinal Chemistry, 页码：4980-4988 , 文章类型： Article，,卷期：2010年53-13] A focused library of furanopyrimidine (350 compounds) was rapidly synthesized in parallel reactors and in situ screened for Aurora and epidermal growth factor receptor (EGFR) kinase activity, leading to the identificatio... 6-(3,4-Dichlorophenyl)-1-[(Methyloxy)methyl]-3-azabicyclo[4.1.0]heptane: A New Potent and Selective Triple Reuptake Inhibitor [作者：MICHELI FABRIZIO; CAVANNI PAOLO; ANDREOTTI DANIELE; ARBAN ROBERTO; BENEDETTI ROBERTO; BERTANI BARBARA; BETTATI MICHELA; BETTELINI LETIZIA; BONANOMI GIORGIO; BRAGGIO SIMONE; CARLETTI RENZO; CHECCHIA ANNA; CORSI MAURO; FAZZOLARI ELETTRA; FONTANA STEFANO; MARCHIORO CARLA; MERLOPICH EMILIO; NEGRI MICHELE; OLIOSI BEATRICE; RATTI EMILIANGELO; READ KEVIN D; ROSCIC MAJA; SARTORI ILARIA; SPADA SIMONE; TEDESCO GIOVANNA; TARSI LUCA; TERRENI SILVIA; VISENTINI FILIPPO; ZOCCHI ALESSANDRO; ZONZINI LAURA; DI FABIO ROMANO,期刊：Journal of Medicinal Chemistry, 页码：4989-5001 , 文章类型： Article，,卷期：2010年53-13] A pharmacophore model for triple reuptake inhibitors and the new class of 1-(aryl)-6-[alkoxyalkyl]-3-azabicyclo[3.1.0]hexanes were recently reported. Further investigation in this area led to the identification of a new ... Scaffold Explorer: An Interactive Tool for Organizing and Mining Structure-Activity Data Spanning Multiple Chemotypes [作者：AGRAFIOTIS DIMITRIS K; WIENER JOHN J M,期刊：Journal of Medicinal Chemistry, 页码：5002-5011 , 文章类型： Article，,卷期：2010年53-13] We introduce Scaffold Explorer, an interactive tool that allows medicinal chemists to define hierarchies of chemical scaffolds and use them to explore their project data. Scaffold Explorer allows the user to construct a ... Design, Synthesis, and Structure-Activity Relationship Studies of Novel 2,4,6-Trisubstituted-5-pyrimidinecarboxylic Acids as Peroxisome Proliferator-Activated Receptor gamma (PPAR gamma) Partial Agonists with Comparable Antidiabetic Efficacy to Rosiglitazone [作者：SETO SHIGEKI; OKADA KYOKO; KIYOTA KOICHI; ISOGAI SHIGEKI; IWAGO MAKI; SHINOZAKI TAKEHIRO; KITAMURA YOSHIAKI; KOHNO YASUSHI; MURAKAMI KOJI,期刊：Journal of Medicinal Chemistry, 页码：5012-5024 , 文章类型： Article，,卷期：2010年53-13] A series of novel 2,4,6-trisubstitutedpyrimidine-5-carboxylic acid derivatives were designed and synthesized with the intent of producing a peroxisome proliferator-activated receptor gamma (PPAR gamma) partial agonist fo... Computer-Aided Identification of Trypanosoma brucei Uridine Diphosphate Galactose 4 '-Epimerase Inhibitors: Toward the Development of Novel Therapies for African Sleeping Sickness [作者：DURRANT JACOB D; URBANIAK MICHAEL D; FERGUSON MICHAEL A J; MCCAMMON J ANDREW,期刊：Journal of Medicinal Chemistry, 页码：5025-5032 , 文章类型： Article，,卷期：2010年53-13] Trypanosoma brucei, the causative agent of human African trypanosomiasis, affects tens of thousands of sub-Saharan Africans. As current therapeutics are inadequate due to toxic side effects, drug resistance, and limited ... Selective Synthesis and Biological Evaluation of Sulfate-Conjugated Resveratrol Metabolites [作者：HOSHINO JUMA; PARK EUNJUNG; KONDRATYUK TAMARA P; MARLER LAURA; PEZZUTO JOHN M; VAN BREEMEN RICHARD B; MO SHUNYAN; LI YONGCHAO; CUSHMAN MARK,期刊：Journal of Medicinal Chemistry, 页码：5033-5043 , 文章类型： Article，,卷期：2010年53-13] Five resveratrol sulfate metabolites were synthesized and assessed for activities known to be mediated by resveratrol: inhibition of tumor necrosis factor (TNF)alpha induced NF kappa B activity, cylcooxygenases (COX-1 an... Bivalent Diketopiperazine-Based Tropomysin Receptor Kinase C (TrkC) Antagonists [作者：LIU JING; BRAHIMI FOUAD; SARAGOVI H URI; BURGESS KEVIN,期刊：Journal of Medicinal Chemistry, 页码：5044-5048 , 文章类型： Article，,卷期：2010年53-13] Bivalent molecules containing two beta-turn mimics with side chains that correspond to hot-spots on the neurotrophin NT-3 were prepared. Binding assays showed the mimetics to be selective TrkC ligands, and biological ass... Isopropylidene Substitution Increases Activity and Selectivity of Biphenylmethylene 4-Pyridine Type CYP17 Inhibitors [作者：HU QINGZHONG; YIN LINA; JAGUSCH CARSTEN; HILLE ULRIKE E; HARTMANN ROLF W,期刊：Journal of Medicinal Chemistry, 页码：5049-5053 , 文章类型： Article，,卷期：2010年53-13] GYP 17 inhibition is a promising therapy for prostate cancer (PC) because proliferation of 80% of PC depends on androgen stimulation. Introduction of isopropylidene substituents onto the linker of biphenylmethylene 4-pyr... Kinesin Spindle Protein (KSP) Inhibitors with 2,3-Fused Indole Scaffolds [作者：OISHI SHINYA; WATANABE TOSHIAKI; SAWADA JUNICHI; ASAI AKIRA; OHNO HIROAKI; FUJII NOBUTAKA,期刊：Journal of Medicinal Chemistry, 页码：5054-5058 , 文章类型： Article，,卷期：2010年53-13] Mitotic kinesin spindle protein (KSP) is involved in the assembly of the bipolar spindle during cell division. On the basis of a common 2,3-fused indole substructure within the complex frameworks of terpendole E and othe... Host-Guest Chemistry of the Peptidoglycan [作者：FISHER JED F; MOBASHERY SHAHRIAR,期刊：Journal of Medicinal Chemistry, 页码：4813-4829 , 文章类型： Article，,卷期：2010年53-13] Cheminformatic Tools for Medicinal Chemists [作者：MUCHMORE STEVEN W; EDMUNDS JEREMY J; STEWART KENT D; HAJDUK PHILIP J,期刊：Journal of Medicinal Chemistry, 页码：4830-4841 , 文章类型： Article，,卷期：2010年53-13] Cytotoxicity of Artesunic Acid Homo- and Heterodimer Molecules toward Sensitive and Multidrug-Resistant CCRF-CEM Leukemia Cells [作者：HORWEDEL CINDY; TSOGOEVA SVETLANA B; WEI SHENGWEI; EFFERTH THOMAS,期刊：Journal of Medicinal Chemistry, 页码：4842-4848 , 文章类型： Article，,卷期：2010年53-13] A novel approach to circumvent multidrug resistance is hybridization of natural products in dimers. We analyzed homodimers of two artesunic acid molecules and heterohybrids of artesunic acid and betulin in human CCRF-CEM... Amphiphilic Amide Nitrones: A New Class of Protective Agents Acting as Modifiers of Mitochondrial Metabolism [作者：DURAND GREGORY; POEGGELER BURKHARD; ORTIAL STEPHANIE; POLIDORI ANGE; VILLAMENA FREDERICK A; BOEKER JUTTA; HARDELAND RUEDIGER; PAPPOLLA MIGUEL A; PUCCI BERNARD,期刊：Journal of Medicinal Chemistry, 页码：4849-4861 , 文章类型： Article，,卷期：2010年53-13] Our group has demonstrated that the amphiphilic character of alpha-phenyl-N-tert-butyl nitrone based agents is a key feature in determining their bioactivity and protection against oxidative toxicity. In this work, we re...