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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29条记录   Public Domain Databases for Medicinal Chemistry [作者：NICOLA GEORGE; LIU TIQING; GILSON MICHAEL K,期刊：Journal of Medicinal Chemistry, 页码：6987-7002 , 文章类型： Article，,卷期：2012年55-16] Lessons from Natural Products Chemistry Can Offer Novel Approaches for Synthetic Chemistry in Drug Discovery Miniperspective [作者：VASILEVICH NATALYA I; KOMBAROV ROMAN V; GENIS DMITRY V; KIRPICHENOK MICHAEL A,期刊：Journal of Medicinal Chemistry, 页码：7003-7009 , 文章类型： Article，,卷期：2012年55-16] Identifying Novel Adenosine Receptor Ligands by Simultaneous Proteochemometric Modeling of Rat and Human Bioactivity Data [作者：VAN WESTEN GERARD J P; VAN DEN HOVEN OLAF O; VAN DER PIJL RIANNE; MULDERKRIEGER THEA; DE VRIES HENK; WEGNER JORG K; IJZERMAN ADRIAAN P; VAN VLIJMEN HERMAN W T; BENDER ANDREAS,期刊：Journal of Medicinal Chemistry, 页码：7010-7020 , 文章类型： Article，,卷期：2012年55-16] The four subtypes of adenosine receptors form relevant drug targets in the treatment of, e.g., diabetes and Parkinson's disease. In the present study, we aimed at finding novel small molecule ligands for these receptors ... Discovery of Piragliatin-First Glucokinase Activator Studied in Type 2 Diabetic Patients [作者：SARABU RAMAKANTH; BIZZARRO FRED T; CORBETT WENDY L; DVOROZNIAK MARK T; GENG WANPING; GRIPPO JOSEPH F; HAYNES NANCYELLEN; HUTCHINGS STANLEY; GAROFALO LISA; GUERTIN KEVIN R; HILLIARD DARRYL W; KABAT MAREK; KESTER ROBERT F; KA WANG; LIANG ZHENMIN; MAHANEY PAIGE E; MARCUS LINDA; MATSCHINSKY FRANZ M; MOORE DAVID; RACHA JAGDISH; RADINOV ROUMEN; REN YI; QI LIDA; PIGNATELLO MICHAEL; SPENCE CHERYL L; STEELE THOMAS; TENGI JOHN; GRIMSBY JOSEPH,期刊：Journal of Medicinal Chemistry, 页码：7021-7036 , 文章类型： Article，,卷期：2012年55-16] Glucokinase (GK) activation as a potential strategy to treat type 2 diabetes (T2D) is well recognized. Compound 1, a glucokinase activator (GKA) lead that we have previously disclosed, caused reversible hepatic lipidosis... Discovery and Optimization of 1,3,4-Trisubstituted-pyrazolone Derivatives as Novel, Potent, and Nonsteroidal Farnesoid X Receptor (FXR) Selective Antagonists [作者：HUANG HUANG; YU YING; GAO ZHENTING; ZHANG YONG; LI CHENJING; XU XING; JIN HUI; YAN WENZHONG; MA RUOQUN; ZHU JIN; SHEN XU; JIANG HUALIANG; CHEN LILI; LI JIAN,期刊：Journal of Medicinal Chemistry, 页码：7037-7053 , 文章类型： Article，,卷期：2012年55-16] LBVS of 12480 in-house compounds, followed by HTRF assay, resulted in one nonsteroidal compound (11) with antagonistic activity against FXR (69.01 +/- 11.75 mu M). On the basis of 11, 26 new derivatives (12a-z) were desi... Shape-Based Reprofiling of FDA-Approved Drugs for the H-1 Histamine Receptor [作者：VASUDEVAN SRIDHAR R; MOORE JOHN B; SCHYMURA YVES; CHURCHILL GRANT C,期刊：Journal of Medicinal Chemistry, 页码：7054-7060 , 文章类型： Article，,卷期：2012年55-16] Reprofiling of existing drugs to treat conditions not originally targeted is an attractive means of addressing the problem of a decreasing stream of approved drugs. To determine if 3D shape similarity can be used to rati... Discovery of Highly Potent and Selective Small Molecule ADAMTS-5 Inhibitors That Inhibit Human Cartilage Degradation via Encoded Library Technology (ELT) [作者：DENG HONGFENG; OKEEFE HEATHER; DAVIE CHRISTOPHER P; LIND KENNETH E; ACHARYA RAKSHA A; FRANKLIN G JOSEPH; LARKIN JONATHAN; MATICO ROSALIE; NEEB MICHAEL; THOMPSON MONIQUE M; LOHR THOMAS; GROSS JEFFREY W; CENTRELLA PAOLO A; ODONOVAN GARY K; BEDARD KATIE L SARGENT; VAN VLOTEN KURT; MATARUSE SIBONGILE; SKINNER STEVEN R; BELYANSKAYA SVETLANA L; CARPENTER TIFFANY Y; SHEARER TODD W; CLARK MATTHEW A; CUOZZO JOHN W; ARICOMUENDEL CHRISTOPHER C; MORGAN BARRY A,期刊：Journal of Medicinal Chemistry, 页码：7061-7079 , 文章类型： Article，,卷期：2012年55-16] The metalloprotease ADAMTS-5 is considered a potential target for the treatment of osteoarthritis. To identify selective inhibitors of ADAMTS-5, we employed encoded library technology (ELT), which enables affinity select... Selective Dual Inhibitors of CYP19 and CYP11B2: Targeting Cardiovascular Diseases Hiding in the Shadow of Breast Cancer [作者：HU QINGZHONG; YIN LINA; HARTMANN ROLF W,期刊：Journal of Medicinal Chemistry, 页码：7080-7089 , 文章类型： Article，,卷期：2012年55-16] Postmenopausal women are at high risk for cardiovascular diseases because of the estrogen deficiency. As for postmenopausal breast cancer patients, this risk is even higher due to inhibition of estrogens biosyntheses in ... Substituent Effects on Desferrithiocin and Desferrithiocin Analogue Iron-Clearing and Toxicity Profiles [作者：BERGERON RAYMOND J; WIEGAND JAN; BHARTI NEELAM; MCMANIS JAMES S,期刊：Journal of Medicinal Chemistry, 页码：7090-7103 , 文章类型： Article，,卷期：2012年55-16] Desferrithiocin (DFT, 1) is a very efficient iron chelator when given orally. However, it is severely nephrotoxic. Structure-activity studies with 1 demonstrated that removal of the aromatic nitrogen to provide desazades... Synthesis and Evaluation of Substituted Chroman-4-one and Chromone Derivatives as Sirtuin 2-Selective Inhibitors [作者：FRIDENSAXIN MARIA; SEIFERT TINA; LANDERGREN MARIE RYDEN; SUURONEN TIINA; LAHTELAKAKKONEN MAIJA; JARHO ELINA M; LUTHMAN KRISTINA,期刊：Journal of Medicinal Chemistry, 页码：7104-7113 , 文章类型： Article，,卷期：2012年55-16] A series of substituted chromone/chroman-4-one derivatives has been synthesized and evaluated as novel inhibitors of SIRT2, an enzyme involved in aging-related diseases, e.g., neurodegenerative disorders. The analogues w... Identification of a Potent Sodium Hydrogen Exchanger Isoform 1 (NHE1) Inhibitor with a Suitable Profile for Chronic Dosing and Demonstrated Cardioprotective Effects in a Preclinical Model of Myocardial Infarction in the Rat [作者：HUBER JOHN D; BENTZIEN JOERG; BOYER STEPHEN J; BURKE JENNIFER; DE LOMBAERT STEPHANE; EICKMEIER CHRISTIAN; GUO XIN; HAIST JAMES V; HICKEY EUGENE R; KAPLITA PAUL; KARMAZYN MORRIS; KEMPER RAYMOND; KENNEDY CHARLES A; KIRRANE THOMAS; MADWED JEFFREY B; MAINOLFI ELIZABETH; NAGARAJA NELAMANGARA; SOLEYMANZADEH FARIBA; SWINAMER ALAN; ELDRUP ANNE B,期刊：Journal of Medicinal Chemistry, 页码：7114-7140 , 文章类型： Article，,卷期：2012年55-16] Sodium-hydrogen exchanger isoform 1 (NHE1) is a ubiquitously expressed transmembrane ion channel responsible for intracellular pH regulation. During myocardial ischemia, low pH activates NHE1 and causes increased intrace... Structure-Functional Selectivity Relationship Studies of beta-Arrestin-Biased Dopamine D-2 Receptor Agonists [作者：CHEN XIN; SASSANO MARIA F; ZHENG LIANYOU; SETOLA VINCENT; CHEN MENG; BAI XU; FRYE STEPHEN V; WETSEL WILLIAM C; ROTH BRYAN L; JIN JIAN,期刊：Journal of Medicinal Chemistry, 页码：7141-7153 , 文章类型： Article，,卷期：2012年55-16] Functionally selective G protein-coupled receptor (GPCR) ligands, which differentially modulate canonical and noncanonical signaling, are extremely useful for elucidating key signal transduction pathways essential for bo... Synthesis and Evaluation of Novel alpha-Fluorinated (E)-3((6-Methylpyridin-2-yl)ethynyl)cyclohex-2-enone-O-methyl Oxime (ABP688) Derivatives as Metabotropic Glutamate Receptor Subtype 5 PET Radiotracers [作者：SEPHTON SELENA MILICEVIC; MU LINJING; SCHWEIZER W BERND; SCHIBLI ROGER; KRAEMER STEFANIE D; AMETAMEY SIMON M,期刊：Journal of Medicinal Chemistry, 页码：7154-7162 , 文章类型： Article，,卷期：2012年55-16] In the search for an optimal fluorine-18-labeled positron emission tomography (PET) radiotracer for imaging metabotropic glutamate receptor subtype 5 (mGluRS), we have prepared a series of five alpha-fluorinated derivati... Antiproliferative and Antimigratory Actions of Synthetic Long Chain n-3 Monounsaturated Fatty Acids in Breast Cancer Cells That Overexpress Cyclooxygenase-2 [作者：CUI PEI H; RAWLING TRISTAN; BOURGET KIRSI; KIM TERRY; DUKE COLIN C; DODDAREDDY MUNIKUMAR R; HIBBS DAVID E; ZHOU FANFAN; TATTAM BRUCE N; PETROVIC NENAD; MURRAY MICHAEL,期刊：Journal of Medicinal Chemistry, 页码：7163-7172 , 文章类型： Article，,卷期：2012年55-16] Cyclooxygenase-2 (COX-2) is overexpressed in many human cancers and converts the n-6 polyunsaturated fatty acid (PUFA) arachidonic acid to prostaglandin E-2 (PGE(2)), which drives tumorigenesis; in contrast, n-3 PUFA inh... Discovery of a Potential Anti-Ischemic Stroke Agent: 3-Pentylbenzo[c]thiophen-1(3H)-one [作者：WU JING; LING JINGJING; WANG XULIANG; LI TINGTING; LIU JINGCHAO; LAI YISHENG; JI HUI; PENG SIXUN; TIAN JIDE; ZHANG YIHUA,期刊：Journal of Medicinal Chemistry, 页码：7173-7181 , 文章类型： Article，,卷期：2012年55-16] The development of novel antithrombotic agents with strong free radical scavenging activity is of great significance for the treatment of ischemic stroke. In the present study, 3-alkyl/arylalkyl-substituted benzo[c]thiop... Revisiting [PtCl2(cis-1,4-DACH)]: An Underestimated Antitumor Drug with Potential Application to the Treatment of Oxaliplatin-Refractory Colorectal Cancer [作者：MARGIOTTA NICOLA; MARZANO CRISTINA; GANDIN VALENTINA; OSELLA DOMENICO; RAVERA MAURO; GABANO ELISABETTA; PLATTS JAMES A; PETRUZZELLA EMANUELE; HOESCHELE JAMES D; NATILE GIOVANNI,期刊：Journal of Medicinal Chemistry, 页码：7182-7192 , 文章类型： Article，,卷期：2012年55-16] Although the encouraging antitumor activity of [PtCl2(cis-1,4-DACH)] (1; DACH = diaminocyclohexane) was shown in early studies almost 20 years ago, the compound has remained nearly neglected. In contrast, oxaliplatin, co...