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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10条记录   N-Alkyl-octahydroisoquinolin-1-one-8-carboxamides: Selective and Nonbasic kappa-Opioid Receptor Ligands [作者：FRANKOWSKI KEVIN J; GHOSH PARTHA; SETOLA VINCENT; TRAN THUY B; ROTH BRYAN L; AUBE JEFFREY,期刊：ACS Medicinal Chemistry Letters, 页码：189-193 , 文章类型： Article，,卷期：2010年1-5] Herein, we report that N-alkyl-octahydroisoquinolin-1-one-8-carboxamides are a novel class of readily synthesized, selective K-opioid receptor (KOR) ligands. A striking feature of this class of compounds is the absence o... Selection, Preparation, and Evaluation of Small-Molecule Inhibitors of Toll-Like Receptor 4 [作者：BEVAN DOUGLAS E; MARTINKO ALEXANDER J; LORAM LISA C; STAHL JOSHUA A; TAYLOR FREDERICK R; JOSHEE SAMPADA; WATKINS LINDA R; YIN HANG,期刊：ACS Medicinal Chemistry Letters, 页码：194-198 , 文章类型： Article，,卷期：2010年1-5] Toll-like receptor 4 (TLR4), a membrane-spanning receptor protein that functions in complex with its accessory protein MD-2, is an intriguing target for therapeutic development. Herein, we report the identification of a ... Allosteric IGF-1R Inhibitors [作者：HEINRICH TIMO; GRAEDLER ULRICH; BOETTCHER HENNING; BLAUKAT ANDREE; SHUTES ADAM,期刊：ACS Medicinal Chemistry Letters, 页码：199-203 , 文章类型： Article，,卷期：2010年1-5] Targeting allosteric protein sites is a promising approach to interfere selectively with cellular signaling cascades. We have discovered a novel class of allosteric insulin-like growth factor-1 receptor (IGF-1R) inhibito... Discovery of Dinaciclib (SCH 727965): A Potent and Selective Inhibitor of Cyclin-Dependent Kinases [作者：PARUCH KAMIL; DWYER MICHAEL P; ALVAREZ CARMEN; BROWN COURTNEY; CHAN TINYAU; DOLL RONALD J; KEERTIKAR KERRY; KNUTSON CHAD; MCKITTRICK BRIAN; RIVERA JOCELYN; ROSSMAN RANDALL; TUCKER GREG; FISCHMANN THIERRY; HRUZA ALAN; MADISON VINCENT; NOMEIR AMIN A; WANG YAOLIN; KIRSCHMEIER PAUL; LEES EMMA; PARRY DAVID; SGAMBELLONE NICOLE; SEGHEZZI WOLFGANG; SCHULTZ LESLEY; SHANAHAN FRANCES; WISWELL DEREK; XU XIAOYING; ZHOU QUIAO; JAMES RAY A; PARADKAR VIDYADHAR M; PARK HAENGSOON; ROKOSZ LAURA R; STAUFFER TARA M; GUZI TIMOTHY J,期刊：ACS Medicinal Chemistry Letters, 页码：204-208 , 文章类型： Article，,卷期：2010年1-5] Inhibition of cyclin-dependent kinases (CDKs) has emerged as an attractive strategy for the development of novel oncology therapeutics. Herein is described the utilization of an in vivo screening approach with integrated... Cobicistat (GS-9350): A Potent and Selective Inhibitor of Human CYP3A as a Novel Pharmacoenhancer [作者：XU LIANHONG; LIU HONGTAO; MURRAY BERNARD P; CALLEBAUT CHRISTIAN; LEE MELODY S; HONG ALLEN; STRICKLEY ROBERT G; TSAI LUONG K; STRAY KIRSTEN M; WANG YUJIN; RHODES GERRY R; DESAI MANOJ C,期刊：ACS Medicinal Chemistry Letters, 页码：209-213 , 文章类型： Article，,卷期：2010年1-5] Cobicistat (3, GS-9350) is a newly discovered, potent, and selective inhibitor of human cytochrome P450 3A (CYP3A) enzymes. In contrast to ritonavir, 3 is devoid of anti-HIV activity and is thus more suitable for use in ... Discovery of a Potent, Injectable Inhibitor of Aurora Kinases Based on the Imidazo-[1,2-a]-Pyrazine Core [作者：YU TAO; TAGAT JAYARAM R; KEREKES ANGELA D; DOLL RONALD J; ZHANG YONGLIAN; XIAO YUSHI; ESPOSITE SARA; BELANGER DAVID B; CURRAN PATRICK J; MANDAL AMIT K; SIDDIQUI M ARSHAD; SHIH NENGYANG; BASSO ANDREA D; LIU MING; GRAY KIMBERLY; TEVAR SEEMA; JONES JENNIFER; LEE SUINING; LIANG LIANZHU; PONERY SAMAD; SMITH ELIZABETH B; HRUZA ALAN; VOIGT JOHANNES; RAMANATHAN LATA; PROSISE WINIFRED; HU MENGWEI,期刊：ACS Medicinal Chemistry Letters, 页码：214-218 , 文章类型： Article，,卷期：2010年1-5] The imidazo-[1,2-a]-pyrazine (1) is a dual inhibitor of Aurora kinases A and B with modest cell potency (IC50 = 250 nM) and low solubility (5 mu M). Lead optimization guided by the binding mode led to the acyclic amino a... Metabolism-Guided Design of Short-Acting Calcium-Sensing Receptor Antagonists [作者：SOUTHERS JAMES A; BAUMAN JONATHAN N; PRICE DAVID A; HUMPHRIES PAUL S; BALAN GAYATRI; SAGAL JOHN F; MAURER TRISTAN S; ZHANG YAN; OLIVER ROBERT; HERR MICHAEL; HEALY DAVID R; LI MEI; KAPINOS BRENDON; FATE GWENDOLYN D; RICCARDI KEITH A; PARALKAR VISHWAS M; BROWN THOMAS A; KALGUTKAR AMIT S,期刊：ACS Medicinal Chemistry Letters, 页码：219-223 , 文章类型： Article，,卷期：2010年1-5] As part of a strategy to deliver short-acting calcium-sensing receptor (CaSR) antagonists, the metabolically labile thiomethyl functionality was incorporated into the zwitterionic amino alcohol derivative 3 with the hope... Synthesis of a Ga-68-Labeled Peptoid-Peptide Hybrid for Imaging of Neurotensin Receptor Expression in Vivo [作者：MASCHAUER SIMONE; EINSIEDEL JUERGEN; HOCKE CARSTEN; HUEBNER HARALD; KUWERT TORSTEN; GMEINER PETER; PRANTE OLAF,期刊：ACS Medicinal Chemistry Letters, 页码：224-228 , 文章类型： Article，,卷期：2010年1-5] The neurotensin receptor subtype 1 (NTS1) represents an attractive molecular target for imaging various tumors. Positron emission tomography (PET) gained widespread importance due to its sensitivity. We combined the desi... Docking to Erlotinib Off-Targets Leads to Inhibitors of Lung Cancer Cell Proliferation with Suitable in Vitro Pharmacokinetics [作者：LI LIWEI; LI JING; KHANNA MAY; JO INHA; BAIRD JASON P; MEROUEH SAMY O,期刊：ACS Medicinal Chemistry Letters, 页码：229-233 , 文章类型： Article，,卷期：2010年1-5] In an effort to develop a rational approach to identify anticancer agents with selective polypharmacology, we mined millions of docked protein ligand complexes involving more than a thousand cancer targets from multiple ... Optimization of an Albumin-Binding Prodrug of Doxorubicin That Is Cleaved by Prostate-Specific Antigen [作者：ELSADEK BAKHEET; GRAESER RALPH; WARNECKE ANDRE; UNGER CLEMENS; SALEEM TAHIA; ELMELEGY NAGLA; MADKOR HAFEZ; KRATZ FELIX,期刊：ACS Medicinal Chemistry Letters, 页码：234-238 , 文章类型： Article，,卷期：2010年1-5] We have developed a novel albumin-binding prodrug of doxorubicin that incorporates p-aminobenzyloxycarbonyl (PABC) as a 1,6 self-immolative spacer in addition to the heptapeptide, Arg-Ser-Ser-Tyr-Tyr-Ser-Leu, as a substr...