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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8条记录   Discovery of an Oral Potent Selective Inhibitor of Hematopoietic Prostaglandin D Synthase (HPGDS) [作者：CARRON CHRIS P; TRUJILLO JOHN I; OLSON KIRK L; HUANG WEI; HAMPER BRUCE C; DICE TOM; NEAL BRADLEY E; PELC MATTHEW J; DAY JACQUELINE E; ROHRER DOUGLAS C; KIEFER JAMES R; MOON JOSEPH B; SCHWEITZER BARBARA A; BLAKE TANISHA D; TURNER STEVE R; WOERNDLE RHONDA; CASE BRENDA L; BONO CHRISTINE P; DILWORTH VICKIE M; FUNCKESSHIPPY CHRISTIE L; HOOD BECKY L; JEROME GINA M; KORNMEIER CHRISTINE M; RADABAUGH MELISSA R; WILLIAMS MELANIE L; DAVIES MICHAEL S; WEGNER CRAIG D; WELSCH DEAN J; ABRAHAM WILLIAM M; WARREN CHAD J; DOWTY MARTIN E; HUA FENGMEI; ZUTSHI ANUP; YANG JERRY Z; THORARENSEN ATLI,期刊：ACS Medicinal Chemistry Letters, 页码：59-63 , 文章类型： Article，,卷期：2010年1-2] Hematopoietic prostaglandin D synthase (HPGDS) is primarly expressed in mast cells, antigen-presenting cells, and Th-2 cells. HPGDS converts PGH(2) into PGD(2), a mediator thought to play a pivotal role in airway allergy... Discovery of Narlaprevir (SCH 900518): A Potent, Second Generation HCV NS3 Serine Protease Inhibitor [作者：ARASAPPAN ASHOK; BENNETT FRANK; BOGEN STEPHANE L; VENKATRAMAN SRIKANTH; BLACKMAN MELISSA; CHEN KEVIN X; HENDRATA SISKA; HUANG YUHUA; HUELGAS REGINA M; NAIR LATHA; PADILLA ANGELA I; PAN WEIDONG; PIKE RUSSELL; PINTO PATRICK; RUAN SUMEI; SANNIGRAHI MOUSUMI; VELAZQUEZ FRANCISCO; VIBULBHAN BANCHA; WU WANLI; YANG WEIYING; SAKSENA ANIL K; GIRIJAVALLABHAN VIYYOOR; SHIH NENGYANG; KONG JIANSHE; MENG TAO; JIN YAN; WONG JESSE; MCNAMARA PAUL; PRONGAY ANDREW; MADISON VINCENT; PIWINSKI JOHN J; CHENG KUOCHI; MORRISON RICHARD; MALCOLM BRUCE; TONG XIAO; RALSTON ROBERT; NJOROGE F GEORGE,期刊：ACS Medicinal Chemistry Letters, 页码：64-69 , 文章类型： Article，,卷期：2010年1-2] Boceprevir (SCH 503034), 1, a novel HCV NS3 serine protease inhibitor discovered in our laboratories, is currently undergoing phase III clinical trials. Detailed investigations toward a second generation protease inhibit... Vorinostat-Like Molecules as Structural, Stereochemical, and Pharmacological Tools [作者：HANESSIAN STEPHEN; AUZZAS LUCIANA; LARSSON ANDREAS; ZHANG JIANBIN; GIANNINI GIUSEPPE; GALLO GRAZIA; CIACCI ANDREA; CABRI WALTER,期刊：ACS Medicinal Chemistry Letters, 页码：70-74 , 文章类型： Article，,卷期：2010年1-2] The inhibitory activity of an omega-alkoxy analogue of the HDAC inhibitor, Vorinostat (SAHA), against the 11 isoforms of HDAC is described and evaluated with regard to structural biology information retrieved through com... Discovery of 4,4-Disubstituted Ouinazolin-2-ones as T-Type Calcium Channel Antagonists [作者：BARROW JAMES C; RITTLE KENNETH E; REGER THOMAS S; YANG ZHIQIANG; BONDISKEY PHUNG; MCGAUGHEY GEORGIA B; BOCK MARK G; HARTMAN GEORGE D; TANG CUYUE; BALLARD JEANINE; KUO YUHSIN; PRUEKSARITANONT THOMAYANT; NUSS CINDY E; DORAN SCOTT M; FOX STEVEN V; GARSON SUSAN L; KRAUS RICHARD L; LI YUXING; MARINO MICHAEL J; GRAUFELDS VALERIE KUZMICK; UEBELE VICTOR N; RENGER JOHN J,期刊：ACS Medicinal Chemistry Letters, 页码：75-79 , 文章类型： Article，,卷期：2010年1-2] A novel series of quinazolinone T-type calcium channel antagonists have been prepared and evaluated using in vitro and in vivo assays. Optimization of the screening hit 3 by modifications of the 3- and 4-positions of the... Synthesis and In Vitro Evaluation of Imidazo[1,2-b]pyridazines as Ligands for beta-Amyloid Plaques [作者：ZENG FANXING; ALAGILLE DAVID; TAMAGNAN GILLES D; CILIAX BRIAN J; LEVEY ALLAN I; GOODMAN MARK M,期刊：ACS Medicinal Chemistry Letters, 页码：80-84 , 文章类型： Article，,卷期：2010年1-2] A series of imidazo[1,2-b]pyridazine derivatives were synthesized and evaluated for binding to amyloid plaques in vitro using synthetic aggregates of A beta(1-40). Binding affinities of these compounds were found to rang... Structure-Based Design of Conformationally Constrained, Cell-Permeable STAT3 Inhibitors [作者：CHEN JIANYONG; BAI LONGCHUAN; BERNARD DENZIL; NIKOLOVSKACOLESKA ZANETA; GOMEZ CINDY; ZHANG JIAN; YI HAN; WANG SHAOMENG,期刊：ACS Medicinal Chemistry Letters, 页码：85-89 , 文章类型： Article，,卷期：2010年1-2] We report herein the structure-based design of a class of conformationally constrained, potent, cell-permeable small-molecule inhibitors to target the SH2 domain in STAT3. Compound 11 (CJ-1383) binds to STAT3 with a K-i ... Strategic Use of Plasma and Microsome Binding To Exploit in Vitro Clearance in Early Drug Discovery [作者：CHANG GEORGE; STEYN STEFANUS J; UMLAND JOHN P; SCOTT DENNIS O,期刊：ACS Medicinal Chemistry Letters, 页码：50-53 , 文章类型： Article，,卷期：2010年1-2] Apparent intrinsic clearance (CLia) determined from microsomal stability assays is a cornerstone in drug discovery. Categorical bins are routinely applied to this end point to facilitate analysis. However, such bins igno... Exploring Target-Selectivity Patterns of Molecular Scaffolds [作者：HU YE; BAJORATH JUERGEN,期刊：ACS Medicinal Chemistry Letters, 页码：54-58 , 文章类型： Article，,卷期：2010年1-2] We investigate the question of whether target-selective molecular scaffolds can be identified on the basis of currently available compound activity data. Starting from a pool of 17745 public domain compounds with activit...