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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49条记录   Selective Class I Phosphoinositide 3-Kinase Inhibitors: Optimization of a Series of Pyridyltriazines Leading to the Identification of a Clinical Candidate, AMG 511 [作者：NORMAN MARK H; ANDREWS KRISTIN L; BO YUNXIN Y; BOOKER SHON K; CAENEPEEL SEAN; CEE VICTOR J; DANGELO NOEL D; FREEMAN DANIEL J; HERBERICH BRADLEY J; HONG FANGTSAO; JACKSON CLAIRE L M; JIANG JIAN; LANMAN BRIAN A; LIU LONGBIN; MCCARTER JOHN D; MULLADY ERIN L; NISHIMURA NOBUKO; PETTUS LIPING H; REED ANTHONY B; MIGUEL TISHA SAN; SMITH ADRIAN L; STEC MARKIAN M; TADESSE SEIFU; TASKER ANDREW; AIDASANI DIVESH; ZHU XIAOCHUN; SUBRAMANIAN RAJU; TAMAYO NURIA A; WANG LING; WHITTINGTON DOUGLAS A; WU BIN; WU TIAN; WURZ RYAN P; YANG KEVIN; ZALAMEDA LEEANNE; ZHANG NANCY; HUGHES PAUL E,期刊：Journal of Medicinal Chemistry, 页码：7796-7816 , 文章类型： Article，,卷期：2012年55-17] The phosphoinositide 3-kinase family catalyzes the phosphorylation of phosphatidylinositol-4,5-diphosphate to phosphatidylinositol-3,4,5-triphosphate, a secondary messenger which plays a critical role in important cellul... Synthesis, Aqueous Reactivity, and Biological Evaluation of Carboxylic Acid Ester-Functionalized Platinum-Acridine Hybrid Anticancer Agents [作者：GRAHAM LEIGH A; SURYADI JIMMY; WEST TIFFANY K; KUCERA GREGORY L; BIERBACH ULRICH,期刊：Journal of Medicinal Chemistry, 页码：7817-7827 , 文章类型： Article，,卷期：2012年55-17] The synthesis of platinum-acridine hybrid agents containing carboxylic acid ester groups is described. The most active derivatives and the unmodified parent compounds showed up to 6-fold higher activity in ovarian cancer... Discovery of Tofogliflozin, a Novel C-Arylglucoside with an O-Spiroketal Ring System, as a Highly Selective Sodium Glucose Cotransporter 2 (SGLT2) Inhibitor for the Treatment of Type 2 Diabetes [作者：OHTAKE YOSHIHITO; SATO TSUTOMU; KOBAYASHI TAKAMITSU; NISHIMOTO MASAHIRO; TAKA NAOKI; TAKANO KOJI; YAMAMOTO KEISUKE; OHMORI MASAYUKI; YAMAGUCHI MARINA; TAKAMI KYOKO; YEU SANGYONG; AHN KOOHYEON; MATSUOKA HIROHARU; MORIKAWA KAZUMI; SUZUKI MASAYUKI; HAGITA HITOSHI; OZAWA KAZUHARU; YAMAGUCHI KOJI; KATO MOTOHIRO; IKEDA SACHIYA,期刊：Journal of Medicinal Chemistry, 页码：7828-7840 , 文章类型： Article，,卷期：2012年55-17] Inhibition of sodium glucose cotransporter 2 (SGLT2) has been proposed as a novel therapeutic approach to treat type 2 diabetes. In our efforts to discover novel inhibitors of SGLT2, we first generated a 3D pharmacophore... Crystal Structure of Human Aurora B in Complex with INCENP and VX-680 [作者：ELKINS JONATHAN M; SANTAGUIDA STEFANO; MUSACCHIO ANDREA; KNAPP STEFAN,期刊：Journal of Medicinal Chemistry, 页码：7841-7848 , 文章类型： Article，,卷期：2012年55-17] We present the structure of the human Aurora B kinase domain in complex with the C-terminal Aurora-binding region of human INCENP and the Aurora kinase inhibitor VX-680. The structure unexpectedly reveals a dimeric arran... The Discovery of N-[5-(4-Bromophenyl)-6-[2-[(5-bromo-2-pyrimidinyl)oxy]ethoxy]-4-pyrimidi nyl]-N '-propylsulfamide (Macitentan), an Orally Active, Potent Dual Endothelin Receptor Antagonist [作者：BOLLI MARTIN H; BOSS CHRISTOPH; BINKERT CHRISTOPH; BUCHMANN STEPHAN; BUR DANIEL; HESS PATRICK; IGLARZ MARC; MEYER SOLANGE; REIN JOSIANE; REY MARKUS; TREIBER ALEXANDER; CLOZEL MARTINE; FISCHLI WALTER; WELLER THOMAS,期刊：Journal of Medicinal Chemistry, 页码：7849-7861 , 文章类型： Article，,卷期：2012年55-17] Starting from the structure of bosentan (1), we embarked on a medicinal chemistry program aiming at the identification of novel potent dual endothelin receptor antagonists with high oral efficacy. This led to the discove... Targeting the Hinge Glycine Flip and the Activation Loop: Novel Approach to Potent p38 alpha Inhibitors [作者：MARTZ KATHRIN E; DORN ANGELIKA; BAUR BENJAMIN; SCHATTEL VERENA; GOETTERT MARCIA I; MAYERWRANGOWSKI SVENJA C; RAUH DANIEL; LAUFER STEFAN A,期刊：Journal of Medicinal Chemistry, 页码：7862-7874 , 文章类型： Article，,卷期：2012年55-17] The p38 MAP kinase is a key player in signaling pathways regulating the biosynthesis of inflammatory cytokines. Small molecule p38 inhibitors suppress the production of these cytokines. Therefore p38 is a promising drug ... Carbamoylphosphonates Control Tumor Cell Proliferation and Dissemination by Simultaneously Inhibiting Carbonic Anhydrase IX and Matrix Metalloproteinase-2. Toward Nontoxic Chemotherapy Targeting Tumor Microenvironment [作者：REICH REUVEN; HOFFMAN AMNON; VEERENDHAR AINELLY; MARESCA ALFONSO; INNOCENTI ALESSIO; SUPURAN CLAUDIU T; BREUER ELI,期刊：Journal of Medicinal Chemistry, 页码：7875-7882 , 文章类型： Article，,卷期：2012年55-17] Carbamoylphosphonates (CPOs) have been identified as inhibitors of matrix metalloproteinases (MMPs) and as orally active, bioavailable, and safe antimetastatic agents. In this article, we focus on the direct antitumor ac... Synthesis and Biological Investigations of Nitric Oxide Releasing Nateglinide and Meglitinide Type II Antidiabetic Prodrugs: In-Vivo Antihyperglycemic Activities and Blood Pressure Lowering Studies [作者：KAUR JATINDER; BHARDWAJ ATUL; HUANG ZHANGJIAN; NARANG DEEPAK; CHEN TINGYUEH; PLANE FRANCES; KNAUS EDWARD E,期刊：Journal of Medicinal Chemistry, 页码：7883-7891 , 文章类型： Article，,卷期：2012年55-17] A new group of hybrid nitric oxide-releasing type II antidiabetic drugs possessing a 1-(pyrrolidin-1-yl)diazen-1-ium-1,2-diolate (13 and 18), 1-(N,N-diethylamino)diazen-1-ium-1,2-diolate (14 and 19), or nitrooxyethyl (15... Malaria-Infected Mice Live Until at Least Day 30 after a New Artemisinin-Derived Thioacetal Thiocarbonate Combined with Mefloquine Are Administered Together in a Single, Low, Oral Dose [作者：JACOBINE ALEXANDER M; MAZZONE JENNIFER R; SLACK RACHEL D; TRIPATHI ABHAI K; SULLIVAN DAVID J; POSNER GARY H,期刊：Journal of Medicinal Chemistry, 页码：7892-7899 , 文章类型： Article，,卷期：2012年55-17] In only three steps and in 21-67% overall yields from the natural trioxane artemisinin, a series of 21 new trioxane C-10 thioacetals was prepared. Upon receiving a single oral dose of only 6 mg/kg of the monomeric trioxa... Synthesis and Evaluation of Silanediols as Highly Selective Uncompetitive Inhibitors of Human Neutrophil Elastase [作者：MADSEN JULIE L H; ANDERSEN THOMAS L; SANTAMARIA SALVATORE; NAGASE HIDEAKI; ENGHILD JAN J; SKRYDSTRUP TROELS,期刊：Journal of Medicinal Chemistry, 页码：7900-7908 , 文章类型： Article，,卷期：2012年55-17] Chronic obstructive pulmonary disease (COPD) is an increasing health problem and is estimated to be the fifth leading cause of death in 2020 according to the World Health Organization. Current treatments are only palliat... Toward Rational Fragment-Based Lead Design without 3D Structures [作者：HENEN MORKOS A; COUDEVYLLE NICOLAS; GEIST LEONHARD; KONRAT ROBERT,期刊：Journal of Medicinal Chemistry, 页码：7909-7919 , 文章类型： Article，,卷期：2012年55-17] Fragment-based lead discovery (FBLD) has become a prime component of the armamentarium of modern drug design programs. FBLD identifies low molecular weight ligands that weakly bind to important biological targets. Three-... Discovery of Highly Selective and Orally Active Lysophosphatidic Acid Receptor-1 Antagonists with Potent Activity on Human Lung Fibroblasts [作者：QIAN YIMIN; HAMILTON MATTHEW; SIDDURI ACHYUTHARAO; GABRIEL STEPHEN; REN YONGLIN; PENG RUOQI; KONDRU RAMA; NARAYANAN ARJUN; TRUITT TERRY; HAMID RACHID; CHEN YUN; ZHANG LIN; FRETLAND ADRIAN J; SANCHEZ RUBEN ALVAREZ; CHANG KUNGCHING; LUCAS MATTHEW; SCHOENFELD RYAN C; LAINE DRAMANE; FUENTES MARIA E; STEVENSON CHRISTOPHER S; BUDD DAVID C,期刊：Journal of Medicinal Chemistry, 页码：7920-7939 , 文章类型： Article，,卷期：2012年55-17] Lysophosphatidic acid is a class of bioactive phospholipid that mediates most of its biological effects through LPA receptors, of which six isoforms have been identified. The recent results from LPA1 knockout mice sugges... Identification of Antitubercular Benzothiazinone Compounds by Ligand-Based Design [作者：KAROLI TOMISLAV; BECKER BERND; ZUEGG JOHANNES; MOELLMANN UTE; RAMU SOUMYA; HUANG JOHNNY X; COOPER MATTHEW A,期刊：Journal of Medicinal Chemistry, 页码：7940-7944 , 文章类型： Article，,卷期：2012年55-17] 1,3-Benzothiazin-4-ones (BTZs) are a novel class of TB drug candidates with potent activity against M. tuberculosis. An in silico ligand-based model based on structure-activity data from 170 BTZ compounds was used to des... Current Landscape of Phosphodiesterase 10A (PDE10A) Inhibition [作者：CHAPPIE THOMAS A; HELAL CHRISTOPHER J; HOU XINJUN,期刊：Journal of Medicinal Chemistry, 页码：7299-7331 , 文章类型： Article，,卷期：2012年55-17] Conformation-Specific Effects of Raf Kinase Inhibitors Miniperspective [作者：WANG XIAOLUN; KIM JOSEPH,期刊：Journal of Medicinal Chemistry, 页码：7332-7341 , 文章类型： Article，,卷期：2012年55-17] Scaling the Druggability Landscape of Human Bromodomains, a New Class of Drug Targets [作者：ZHANG GUANGTAO; SANCHEZ ROBERTO; ZHOU MINGMING,期刊：Journal of Medicinal Chemistry, 页码：7342-7345 , 文章类型： Editorial Material，,卷期：2012年55-17]