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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40条记录   Novel Steroid Inhibitors of Glucose 6-Phosphate Dehydrogenase [作者：HAMILTON NIALL M; DAWSON MARTIN; FAIRWEATHER EMMA E; HAMILTON NICOLA S; HITCHIN JAMES R; JAMES DOMINIC I; JONES STUART D; JORDAN ALLAN M; LYONS AMANDA J; SMALL HELEN F; THOMSON GRAEME J; WADDELL IAN D; OGILVIE DONALD J,期刊：Journal of Medicinal Chemistry, 页码：4431-4445 , 文章类型： Article，,卷期：2012年55-9] Novel derivatives of the steroid DHEA 1, a known uncompetitive inhibitor of G6PD, were designed, synthesized, and tested for their ability to inhibit this dehydrogenase enzyme. Several compounds with approximately 10-fol... Discovery of a Novel Pyrrole Derivative 1-[5-(2-Fluorophenyl)-1-(pyridin-3-ylsulfonyl)-1H-pyrrol-3-yl]-N-methylm ethanamine Fumarate (TAK-438) as a Potassium-Competitive Acid Blocker (P-CAB) [作者：ARIKAWA YASUYOSHI; NISHIDA HARUYULCI; KURASAWA OSAMU; HASUOKA ATSUSHI; HIRASE KEIZO; INATOMI NOBUHIRO; HORI YASUNOBU; MATSUKAWA JUN; IMANISHI AKIO; KONDO MITSUYO; TARUI NAOKI; HAMADA TERUKI; TAKAGI TERUFUMI; TAKEUCHI TOSHIYUKI; KAJINO MASAHIRO,期刊：Journal of Medicinal Chemistry, 页码：4446-4456 , 文章类型： Article，,卷期：2012年55-9] In our pursuit of developing a novel and potent potassium-competitive acid blocker (P-CAB), we synthesized pyrrole derivatives focusing on compounds with low log D and high ligand-lipophilicity efficiency (LLE) values. A... Synthesis and Biological Evaluation of the First Dual Tyrosyl-DNA Phosphodiesterase I (Tdp1)-Topoisomerase I (Top1) Inhibitors [作者：TRUNG XUAN NGUYEN; MORRELL ANDREW; CONDASHERIDAN MARTIN; MARCHAND CHRISTOPHE; AGAMA KELI; BERMINGAM ALUN; STEPHEN ANDREW G; CHERGUI ADEL; NAUMOVA ALENA; FISHER ROBERT; OKEEFE BARRY R; POMMIER YVES; CUSHMAN MARK,期刊：Journal of Medicinal Chemistry, 页码：4457-4478 , 文章类型： Article，,卷期：2012年55-9] Substances with dual tyrosyl-DNA phosphodiesterase I-topoisomerase I inhibitory activity in one low molecular weight compound would constitute a unique class of anticancer agents that could potentially have significant a... Potent Aminocyclitol Glucocerebrosidase Inhibitors are Subnanomolar Pharmacological Chaperones for Treating Gaucher Disease [作者：TRAPERO ANA; GONZALEZBULNES PATRICIA; BUTTERS TERRY D; LLEBARIA AMADEU,期刊：Journal of Medicinal Chemistry, 页码：4479-4488 , 文章类型： Article，,卷期：2012年55-9] Amino-myo-inositol derivatives have been found to be potent inhibitors of glucocerebrosidase (GCase), the beta-glucosidase enzyme deficient in Gaucher disease (GD). When tested using lymphoblasts derived from patients wi... Methyl Effects on Protein-Ligand Binding [作者：LEUNG CHERYL S; LEUNG SIEGFRIED S F; TIRADORIVES JULIAN; JORGENSEN WILLIAM L,期刊：Journal of Medicinal Chemistry, 页码：4489-4500 , 文章类型： Article，,卷期：2012年55-9] The effects of addition of a methyl group to a lead compound on biological activity are examined. A literature analysis of > 2000 cases reveals that an activity boost of a factor of 10 or more is found with an 8% frequen... Novel TEMPO-PEG-RGDs Conjugates Remediate Tissue Damage Induced by Acute Limb Ischemia/Reperfusion [作者：BI WEI; LI XIAOXU; BI YUE; XUE PING; ZHANG YANRONG; GAO XIANG; WANG ZHIBO; LI MENG; ITAGAKI YASUHIRO; BI LANRONG,期刊：Journal of Medicinal Chemistry, 页码：4501-4505 , 文章类型： Article，,卷期：2012年55-9] We have recently developed new Tempo-PEG-RGDs conjugates and have quantitatively examined their antithrombotic and antioxidant capabilities. These compounds were therapeutically beneficial when characterized in both in v... Targeting Peroxisome Proliferator-Activated Receptors (PPARs): Development of Modulators [作者：PIRAT CELINE; FARCE AMAURY; LEBEGUE NICOLAS; RENAULT NICOLAS; FURMAN CHRISTOPHE; MILLET REGIS; YOUS SAID; SPECA SILVIA; BERTHELOT PASCAL; DESREUMAUX PIERRE; CHAVATTE PHILIPPE,期刊：Journal of Medicinal Chemistry, 页码：4027-4061 , 文章类型： Article，,卷期：2012年55-9] Continuous Flow Synthesis. A Pharma Perspective [作者：MALETSANZ LAIA; SUSANNE FLAVIEN,期刊：Journal of Medicinal Chemistry, 页码：4062-4098 , 文章类型： Article，,卷期：2012年55-9] Novel Promising IAP Antagonist on the Horizon for Clinical Translation [作者：FULDA SIMONE,期刊：Journal of Medicinal Chemistry, 页码：4099-4100 , 文章类型： Editorial Material，,卷期：2012年55-9] Discovery of a Potent Small-Molecule Antagonist of Inhibitor of Apoptosis (IAP) Proteins and Clinical Candidate for the Treatment of Cancer (GDC-0152) [作者：FLYGARE JOHN A; BERESINI MAUREEN; BUDHA NAGESHWAR; CHAN HELEN; CHAN IRIS T; CHEETI SRAVANTHI; COHEN FREDERICK; DESHAYES KURT; DOERNER KARL; ECKHARDT S GAIL; ELLIOTT LINDA O; FENG BAINIAN; FRANKLIN MATTHEW C; REISNER STACY FRANKOVITZ; GAZZARD LEWIS; HALLADAY JASON; HYMOWITZ SARAH G; LA HANK; LORUSSO PATRICIA; MAURER BRIGITTE; MURRAY LESLEY; PLISE EMILE; QUAN CLIFFORD; STEPHAN JEANPHILIPPE; YOUNG SHIN G; TOM JEFFREY; TSUI VICKIE; UM JOANNE; VARFOLOMEEV EUGENE; VUCIC DOMAGOJ; WAGNER ANDREW J; WALLWEBER HEIDI J A; WANG LAN; WARE JOSEPH; WEN ZHAOYANG; WONG HARVEY; WONG JONATHAN M; WONG MELISA; WONG SUSAN; YU RON; ZOBEL KERRY; FAIRBROTHER WAYNE J,期刊：Journal of Medicinal Chemistry, 页码：4101-4113 , 文章类型： Article，,卷期：2012年55-9] A series of compounds were designed and synthesized as antagonists of cIAP1/2, ML-IAP, and XIAP based on the N-terminus, AVPI, of mature Smac. Compound 1 (GDC-0152) has the best profile of these compounds; it binds to th... Evaluation of Synthetic FK506 Analogues as Ligands for the FK506-Binding Proteins 51 and 52 [作者：GOPALAKRISHNAN RANGANATH; KOZANY CHRISTIAN; GAALI STEFFEN; KRESS CHRISTOPH; HOOGELAND BASTIAAN; BRACHER ANDREAS; HAUSCH FELIX,期刊：Journal of Medicinal Chemistry, 页码：4114-4122 , 文章类型： Article，,卷期：2012年55-9] The FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Both proteins have been implicated in prostate cancer. Furthermore, single nucleotide polym... Exploration of Pipecolate Sulfonamides as Binders of the FK506-Binding Proteins 51 and 52 [作者：GOPALAKRISHNAN RANGANATH; KOZANY CHRISTIAN; WANG YANSONG; SCHNEIDER SABINE; HOOGELAND BASTIAAN; BRACHER ANDREAS; HAUSCH FELIX,期刊：Journal of Medicinal Chemistry, 页码：4123-4131 , 文章类型： Article，,卷期：2012年55-9] FK506-binding proteins (FKBP) 51 and 52 are cochaperones that modulate the signal transduction of steroid hormone receptors. Single nucleotide polymorphisms in the gene encoding FKBP51 have been associated with a variety... Identification of Small Molecule Inhibitors of the HIV-1 Nucleocapsid-Stem-Loop 3 RNA Complex [作者：WARUI DOUGLAS M; BARANGER ANNE M,期刊：Journal of Medicinal Chemistry, 页码：4132-4141 , 文章类型： Article，,卷期：2012年55-9] Stem-loop 3 RNA (SL3) in psi-RNA is a highly conserved motif in different strains of HIV-1 and serves as a principle determinant for viral packaging. Viral encapsulation is critical for viral replication, and disruption ... Synthesis and Photodynamic Effect of New Highly Photostable Decacationically Armed [60]- and [70]Fullerene Decaiodide Monoadducts To Target Pathogenic Bacteria and Cancer Cells [作者：WANG MIN; HUANG LIYI; SHARMA SULBHA K; JEON SEAHO; THOTA SAMMAIAH; SPERANDIO FELIPE F; NAYKA SUHASINI; CHANG JULIE; HAMBLIN MICHAEL R; CHIANG LONG Y,期刊：Journal of Medicinal Chemistry, 页码：4274-4285 , 文章类型： Article，,卷期：2012年55-9] Novel water-soluble decacationically armed C-60 and C-70 decaiodide monoadducts, C-60- and C-70[>M(C3N6+C3)(2)], were synthesized, characterized, and applied as photosensitizers and potential nano-PDT agents against path... Discovery of Novel 1,2,4-Thiadiazole Derivatives as Potent, Orally Active Agonists of Sphingosine 1-Phosphate Receptor Subtype 1 (S1P(1)) [作者：REN FENG; DENG GUANGHUI; WANG HAILONG; LUAN LINBO; MENG QINGHUA; XU QIONGFENG; XU HENG; XU XUESONG; ZHANG HAIBO; ZHAO BAOWEI; LI CHENGYONG; GUO TAYLOR B; YANG JIANSONG; ZHANG WEI; ZHAO YONGGANG; JIA QIANTAO; LU HONGTAO; XIANG JIANING; ELLIOTT JOHN D; LIN XICHEN,期刊：Journal of Medicinal Chemistry, 页码：4286-4296 , 文章类型： Article，,卷期：2012年55-9] A novel series of 1,2,4-thiadiazole compounds was discovered as selective S1P(1) agonists. The extensive structure-activity relationship studies for these analogues were reported. Among them, 17g was identified to show h... Optimization of Adenosine 5 '-Carboxamide Derivatives as Adenosine Receptor Agonists Using Structure-Based Ligand Design and Fragment Screening [作者：TOSH DILIP K; PHAN KHAI; GAO ZHANGUO; GAKH ANDREI A; XU FEI; DEFLORIAN FRANCESCA; ABAGYAN RUBEN; STEVENS RAYMOND C; JACOBSON KENNETH A; KATRITCH VSEVOLOD,期刊：Journal of Medicinal Chemistry, 页码：4297-4308 , 文章类型： Article，,卷期：2012年55-9] Structures of G protein-coupled receptors (GPCRs) have a proven utility in the discovery of new antagonists and inverse ago fists modulating signaling of this important family of clinical targets. Applicability of active...