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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   Discovery of WAY-260022, a Potent and Selective Inhibitor of the Norepinephrine Transporter [作者：GAVRIN LORI K; MAHANEY PAIGE E; JENKINS DOUGLAS; NOGLE LISA M; MUGFORD CHERYL A; HUSELTON CHRISTINE; LEITER JENNIFER; JOHNSTON GRACE H; BRAY JENIFER A; BURROUGHS KEVIN D; COSMI SCOTT A; ALFINITO PETER; HO DOUGLAS M; DEECHER DARLENE C; TRYBULSKI EUGENE J,期刊：ACS Medicinal Chemistry Letters, 页码：91-95 , 文章类型： Article，,卷期：2010年1-3] The potency and selectivity of a series of 1-{(1S)-2-[amino]-1-3-(trifluoromethoxy)phenyl]ethyl} cyclohexanol analogues are described. These compounds were prepared to improve in vitro metabolic stability and achieve bra... SMARTCyp: A 2D Method for Prediction of Cytochrome P450-Mediated Drug Metabolism [作者：RYDBERG PATRIK; GLORIAM DAVID E; ZARETZKI JED; BRENEMAN CURT; OLSEN LARS,期刊：ACS Medicinal Chemistry Letters, 页码：96-100 , 文章类型： Article，,卷期：2010年1-3] SMARTCyp is an in silico method that predicts the sites of cytochrome P450-mediated metabolism of druglike molecules. The method is foremost a reactivity model, and as such, it shows a preference for predicting sites tha... Highly Selective Inhibitors of Class II Microbial Fructose Bis-phosphate Aldolases [作者：DAHER RACHA; THERISOD MICHEL,期刊：ACS Medicinal Chemistry Letters, 页码：101-104 , 文章类型： Article，,卷期：2010年1-3] We hereby describe the rationale synthesis and biochemical evaluation of the most powerful and selective inhibitors of class II fructose bis-phosphate aldolases so far reported. These inhibitors are of potential therapeu... Preparation and Characterization of Tetrabenazine Enantiomers against Vesicular Monoamine Transporter 2 [作者：YU QIANSHENG; LUO WEIMING; DESCHAMPS JEFFERY; HOLLOWAY HAROLD W; KOPAJTIC THERESA; KATZ JONATHAN L; BROSSI ARNOLD; GREIG NIGEL H,期刊：ACS Medicinal Chemistry Letters, 页码：105-109 , 文章类型： Article，,卷期：2010年1-3] As a clinical medication for the treatment of hyperkinetic movement disorders, in conditions such as Huntington's disease, tetrabenazine (TBZ) has always been used in its racemic form. To establish whether or not its ben... Probing Binding Modes of Small Molecule Inhibitors to the Polo-Box Domain of Human Polo-like Kinase 1 [作者：LIAO CHENZHONG; PARK JUNGEUN; BANG JEONG K; NICKLAUS MARC C; LEE KYUNG S,期刊：ACS Medicinal Chemistry Letters, 页码：110-114 , 文章类型： Article，,卷期：2010年1-3] Purpurogallin (PPG, 2) and poloxin (3) have been reported as inhibitors of the polo-box domain (PBD) of human polo-like kinase 1. However, our experimental results demonstrated that PPG, but not poloxin, binds to the pho... Photodynamic Activity of Liposomal Photosensitizers via Energy Transfer from Antenna Molecules to [60]Fullerene [作者：IKEDA ATSUSHI; AKIYAMA MOTOFUSA; OGAWA TAKUYA; TAKEYA TATSUO,期刊：ACS Medicinal Chemistry Letters, 页码：115-119 , 文章类型： Article，,卷期：2010年1-3] Photodynamic therapy (PDT) is an emerging approach for the treatment of tumor diseases that has received growing interest in the past few years. In this study, we constructed liposomal photosensitizers (PS) for PDT by sh... Discovery and Evaluation of BMS-708163, a Potent, Selective and Orally Bioavailable gamma-Secretase Inhibitor [作者：GILLMAN KEVIN W; STARRETT JOHN E JR; PARKER MICHAEL F; XIE KAI; BRONSON JOANNE J; MARCIN LAWRENCE R; MCELHONE KATE E; BERGSTROM CARL P; MATE ROBERT A; WILLIAMS RICHARD; MEREDITH JERE E JR; BURTON CATHERINE R; BARTEN DONNA M; TOYN JEREMY H; ROBERTS SUSAN B; LENTZ KIMBERLEY A; HOUSTON JOHN G; ZACZEK ROBERT; ALBRIGHT CHARLES F; DECICCO CARL P; MACOR JOHN E; OLSON RICHARD E,期刊：ACS Medicinal Chemistry Letters, 页码：120-124 , 文章类型： Article，,卷期：2010年1-3] During the course of our research efforts to develop a potent and selective gamma-secretase inhibitor for the treatment of Alzheimer's disease, we investigated a series of carboxamide-substituted sulfonamides. Optimizati... Computational Analysis of Protein Hotspots [作者：YANG CHAOYIE; WANG SHAOMENG,期刊：ACS Medicinal Chemistry Letters, 页码：125-129 , 文章类型： Article，,卷期：2010年1-3] Mapping protein hotspots and analysis of the binding free energy associated with each hotspot can provide critical information for drug design. In the present study, we have performed computational analysis for the two k... Discovery of NVP-LDE225, a Potent and Selective Smoothened Antagonist [作者：PAN SHIFENG; WU XU; JIANG JIQING; GAO WENQI; WAN YONGQIN; CHENG DAI; HAN DONG; LIU JUN; ENGLUND NATHAN P; WANG YAN; PEUKERT STEFAN; MILLERMOSLIN KAREN; YUAN JING; GUO RIBO; MATSUMOTO MELISSA; VATTAY ANTHONY; JIANG YUN; TSAO JEFFREY; SUN FANGXIAN; PFERDEKAMPER ANNEMARIE C; DODD STEPHANIE; TUNTLAND TOVE; MANIARA WIESLAWA; KELLEHER JOSEPH F III; YAO YUNGMAE; WARMUTH MARKUS; WILLIAMS JULIET; DORSCH MARION,期刊：ACS Medicinal Chemistry Letters, 页码：130-134 , 文章类型： Article，,卷期：2010年1-3] The blockade of aberrant hedgehog (Hh) signaling has shown promise for therapeutic intervention in cancer. A cell-based phenotypic high-throughput screen was performed, and the lead structure (1) was identified as an inh... Novel Modulator of Na(v)1.1 and Na(v)1.2 Na+ Channels in Rat Neuronal Cells [作者：MAO HUA; FIEBER LYNNE A; GAWLEY ROBERT E,期刊：ACS Medicinal Chemistry Letters, 页码：135-138 , 文章类型： Article，,卷期：2010年1-3] A novel modulator of sodium ion currents was synthesized in 6 steps from a protected dihydroxypyrrolidine nitrone, via 1,3-dipolar cycloaddition reaction with acrylamide. Sodium ion currents in 850 cells were evaluated i...