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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18条记录   Identification of Niclosamide as a New Small-Molecule Inhibitor of the STAT3 Signaling Pathway [作者：REN XIAOMEI; DUAN LEI; HE QIANG; ZHANG ZHANG; ZHOU YI; WU DONGHAI; PAN JINGXUAN; PEI DUANQING; DING KE,期刊：ACS Medicinal Chemistry Letters, 页码：454-459 , 文章类型： Article，,卷期：2010年1-9] Inhibition of the Signal transducer and activator of transcription 3 (STAT3) signaling pathway has been considered a novel therapeutic strategy to treat human cancers with constitutively active STAT3. In this study, we r... Evaluation of Diarylureas for Activity Against Plasmodium falciparum [作者：ZHANG YIQUN; ANDERSON MARC; WEISMAN JENNIFER L; LU MIN; CHOY CINDY J; BOYD VINCENT A; PRICE JEANINE; SIGAL MARTINA; CLARK JULIE; CONNELLY MICHELE; ZHU FANGYI; GUIGUEMDE W ARMAND; JEFFRIES CYNTHIA; YANG LEI; LEMOFF ANDREW; LIOU ALLY P; WEBB THOMAS R; DERISI JOSEPH L; GUY R KIPLIN,期刊：ACS Medicinal Chemistry Letters, 页码：460-465 , 文章类型： Article，,卷期：2010年1-9] A library of diarylurea insulin-like growth factor 1 receptor inhibitors was screened for activity against chloroquine-sensitive (3D7) and chloroquine-resistant (K1) strains of Plasmodium falciparum. The 4-aminoquinaldin... Pyridine Carboxamides: Potent Palm Site Inhibitors of HCV NS5B Polymerase [作者：CHENG CLIFF C; HUANG XIAOHUA; SHIPPS GERALD W JR; WANG YUSEN; WYSS DANIEL F; SOUCY KYLE A; JIANG CHUANKUI; AGRAWAL SONY; FERRARI ERIC; HE ZHIQING; HUANG HC,期刊：ACS Medicinal Chemistry Letters, 页码：466-471 , 文章类型： Article，,卷期：2010年1-9] Pyridine carboxamide-based inhibitors of the hepatitis C virus (HCV) NS5B polymerase were diversified and optimized to a variety of topologically related scaffolds. In particular, the 2-methyl nicotinic acid scaffold was... Discovery of Omecamtiv Mecarbil the First, Selective, Small Molecule Activator of Cardiac Myosin [作者：MORGAN BRADLEY P; MUCI ALEXANDER; LU PUPING; QIAN XIANGPING; TOCHIMOTO TODD; SMITH WHITNEY W; GARARD MARC; KRAYNACK ERICA; COLLIBEE SCOTT; SUEHIRO ION; TOMASI ADAM; VALDEZ S COREY; WANG WENYUE; JIANG HONG; HARTMAN JAMES; RODRIGUEZ HECTOR M; KAWAS RAJA; SYLVESTER SHEILA; ELIAS KATHLEEN A; GODINEZ GUILLERMO; LEE KENNETH; ANDERSON ROBERT; SUEOKA SANDRA; XU DONGHONG; WANG ZHENGPING; DJORDJEVIC NEBOJSA; MALIK FADY I; MORGANS DAVID J JR,期刊：ACS Medicinal Chemistry Letters, 页码：472-477 , 文章类型： Article，,卷期：2010年1-9] We report the design, synthesis, and optimization of the first, selective activators of cardiac myosin. Starting with a poorly soluble, nitroaromatic hit compound (1), potent, selective, and soluble myosin activators wer... A Potent and Selective AMPK Activator That Inhibits de Novo Lipogenesis [作者：GOMEZGALENO JORGE E; DANG QUN; NGUYEN THANH H; BOYER SERGE H; GROTE MATTHEW P; SUN ZHILI; CHEN MINGWEI; CRAIGO WILLIAM A; VAN POELJE PAUL D; MACKENNA DEIDRE A; CABLE EDWARD E; ROLZIN PAUL A; FINN PATRICIA D; CHI BERT; LINEMEYER DAVID L; HECKER SCOTT J; ERION MARK D,期刊：ACS Medicinal Chemistry Letters, 页码：478-482 , 文章类型： Article，,卷期：2010年1-9] AMP-activated protein kinase (AMPK) is a heterotrimeric kinase that regulates cellular. energy metabolism by affecting energy-consuming pathways such as de novo. lipid biosynthesis and glucose production as well as energ... Discovery of INCB9471, a Potent, Selective, and Orally Bioavailable CCR5 Antagonist with Potent Anti-HIV-1 Activity [作者：XUE CHUBIAO; CHEN LIHUA; CAO GANFENG; ZHANG KE; WANG ANLAI; MELONI DAVID; GLENN JOSEPH; ANAND RAJAN; XIA MICHAEL; KONG LING; HUANG TAISHENG; FENG HAO; ZHENG CHANGSHENG; LI MEI; GALYA LAURINE; ZHOU JIACHENG; SHIN NIU; BARIBAUD FREDRIC; SOLOMON KIM; SCHERLE PEGGY; ZHAO BITAO; DIAMOND SHARON; EMM TOM; KELLER DOUGLAS; CONTEL NANCY; YELESWARAM SWAMY; VADDI KRIS; HOLLIS GREGORY; NEWTON ROBERT; FRIEDMAN STEVEN; METCALF BRIAN,期刊：ACS Medicinal Chemistry Letters, 页码：483-487 , 文章类型： Article，,卷期：2010年1-9] To identify a CCR5 antagonist as an HIV-1 entry inhibitor, we designed a novel series of indane derivatives based on conformational considerations. Modification on the indane ring led to the discovery of compound 22a (IN... Discovery of Dual VEGFR-2 and Tubulin Inhibitors with in Vivo Efficacy [作者：CHEKLER EUGENE L PIATNITSKI; KISELYOV ALEXANDER S; OUYANG XIAOHU; CHEN XIAOLING; PATTAROPONG VATEE; WANG YING; TUMA M CAROLINA; DOODY JACQUELINE F,期刊：ACS Medicinal Chemistry Letters, 页码：488-492 , 文章类型： Article，,卷期：2010年1-9] In an effort to develop potent, orally bioavailable compounds for the treatment of neoplastic diseases, we developed a class of dual VEGFR-2 kinase and tubulin inhibitors. Targeting the VEGFR receptor kinase and tubulin ... Discovery of a Potent Inhibitor of Anaplastic Lymphoma Kinase with in Vivo Antitumor Activity [作者：OTT GREGORY R; TRIPATHY RABINDRANATH; CHENG MANGENG; MCHUGH ROBERT; ANZALONE ANDREW V; UNDERINER TED L; CURRY MATTHEW A; QUAIL MATTHEW R; LU LIHUI; WAN WEIHUA; ANGELES THELMA S; ALBOM MARK S; AIMONE LISA D; ATOR MARK A; RUGGERI BRUCE A; DORSEY BRUCE D,期刊：ACS Medicinal Chemistry Letters, 页码：493-498 , 文章类型： Article，,卷期：2010年1-9] A series of novel 7-amino-1,3,4,5-tetrahydrobenzo[b]azepin-2-one derivatives within the diaminopyrimidine class of kinase inhibitors were identified that target anaplastic lymphoma kinase (ALK). These inhibitors are pote... Design of a High Fragment Efficiency Library by Molecular Graph Theory [作者：VENHORST JENNIFER; NUNEZ SARA; KRUSE CHRIS G,期刊：ACS Medicinal Chemistry Letters, 页码：499-503 , 文章类型： Article，,卷期：2010年1-9] Molecular graph theory was used to design a unique and diverse, high-efficiency fragment screening collection. A data set retrieved from the annotated database AurSCOPE GPS was used as the reference set, and the GDB-13 d... Short-Acting T-Type Calcium Channel Antagonists Significantly Modify Sleep Architecture in Rodents [作者：YANG ZHIQIANG; SCHLEGEL KELLYANN S; SHU YOUHENG; REGER THOMAS S; CUBE ROWENA; MATTERN CHRISTA; COLEMAN PAUL J; SMALL JIM; HARTMAN GEORGE D; BALLARD JEANINE; TANG CUYUE; KUO YUHSIN; PRUEKSARITANONT THOMAYANT; NUSS CINDY E; DORAN SCOTT; FOX STEVE V; GARSON SUSAN L; LI YUXING; KRAUS RICHARD L; UEBELE VICTOR N; TAYLOR ADEKEMI B; ZENG WEI; FANG WEI; CHAVEZENG CYNTHIA; TROYER MATTHEW D; LUK JULIE ANN; LAETHEM TINE; COOK WILLIAM O; RENGER JOHN J; BARROW JAMES C,期刊：ACS Medicinal Chemistry Letters, 页码：504-509 , 文章类型： Article，,卷期：2010年1-9] A novel phenyl acetamide series of short-acting T-type calcium channel antagonists has been identified and evaluated using in vitro and in vivo assays. Heterocycle substitutions of the 4-position of the phenyl acetamides... Discovery of an Orally Efficacious Imidazo[5,1-f][1,2,4]triazine Dual Inhibitor of IGF-1R and IR [作者：JIN MEIZHONG; GOKHALE PRAFULLA C; COOKE ANDY; FOREMAN KENNETH; BUCK ELIZABETH; MAY EARL W; FENG LIXIN; BITTNER MARK A; KADALBAJOO MRIDULA; LANDFAIR DARLA; SIU KAM W; STOLZ KATHRYN M; WERNER DOUGLAS S; LAUFER RADOSLAW S; LI ANHU; DONG HANQING; STEINIG ARNO G; KLEINBERG ANDREW; YAO YAN; PACHTER JONATHAN A; WILD ROBERT; MULVIHILL MARK J,期刊：ACS Medicinal Chemistry Letters, 页码：510-515 , 文章类型： Article，,卷期：2010年1-9] This report describes the investigation of a series of 5,7-disubstituted imidazo[5,1-f][1,2,4]triazine inhibitors of insulin-like growth factor-1 receptor (IGF-1R) and insulin receptor (IR). Structure-activity relationsh... Discovery of A New Human A(2A) Adenosine Receptor Agonist, Truncated 2-Hexynyl-4 '-thioadenosine [作者：HOU XIYAN; KIM HEA OK; ALEXANDER VARUGHESE; KIM KYUNGLIM; CHOI SUN; PARK SEULGI; LEE JIN HEE; YOO LENA S; GAO ZHANGUO; JACOBSON KENNETH A; JEONG LAK SHIN,期刊：ACS Medicinal Chemistry Letters, 页码：516-520 , 文章类型： Article，,卷期：2010年1-9] The truncated C2- and C8-substituted 4'-thioadenosine derivatives 4a-d were synthesized from D-mannose, using palladium-Catalyzed cross-coupling reactions as key steps. In this study, an A(3) adenosine receptor. (AR) ant... Modification at the Lipophilic Domain of RXR Agonists Differentially Influences Activation of RXR Heterodimers [作者：OHSAWA FUMINORI; MORISHITA KENICHI; YAMADA SHOYA; MAKISHIMA MAKOTO; KAKUTA HIROKI,期刊：ACS Medicinal Chemistry Letters, 页码：521-525 , 文章类型： Article，,卷期：2010年1-9] RXR permissive heterodimers are reported to be activated differently depending upon the chemical structure of RXR agonists, but the relationship of agonist structure to differential heterodimer activation has not been ex... Benzimidazole-2-pyrazole HIF Prolyl 4-Hydroxylase Inhibitors as Oral Erythropoietin Secretagogues [作者：ROSEN MARK D; VENKATESAN HARIHARAN; PELTIER HILLARY M; BEMBENEK SCOTT D; KANELAKIS KIMON C; ZHAO LUCY X; LEONARD BARRY E; HOCUTT FRANCES M; WU XIAODONG; PALOMINO HEATHER L; BRONDSTETTER THERESA I; HAUGH PETER V; CAGNON LAURENCE; YAN WEN; LIOTTA LISA A; YOUNG ANDREW; MIRZADEGAN TARA; SHANKLEY NIGEL P; BARRETT TERRANCE D; RABINOWITZ MICHAEL H,期刊：ACS Medicinal Chemistry Letters, 页码：526-529 , 文章类型： Article，,卷期：2010年1-9] HIF prolyl 4-hydroxylases (PHD) are a family of enzymes that mediate key physiological responses to hypoxia by modulating the levels of hypoxia inducible factor 1-alpha (HIF1 alpha). Certain benzimidazole-2-pyrazole carb... Design, Synthesis, and in Vitro Evaluation of Novel Aminomethyl-pyridines as DPP-4 Inhibitors [作者：KACZANOWSKA KATARZYNA; WIESMUELLER KARLHEINZ; SCHAFFNER ARNAUDPIERRE,期刊：ACS Medicinal Chemistry Letters, 页码：530-535 , 文章类型： Article，,卷期：2010年1-9] A collection of novel aminomethyl-pyridines was designed, synthesized, and investigated as potential inhibitors of DPP-4. Optimization of the screening hit afforded a number of 5-aminomethyl-pyridines with inhibitory act... Facile Synthesis of a Fluorescent Cyclosporin A Analogue To Study Cyclophilin 40 and Cyclophilin 18 Ligands [作者：GAALI STEFFEN; KOZANY CHRISTIAN; HOOGELAND BASTIAAN; KLEIN MARIELLE; HAUSCH FELIX,期刊：ACS Medicinal Chemistry Letters, 页码：536-539 , 文章类型： Article，,卷期：2010年1-9] There are strong indications for the involvement of cyclophilin 40 in diseases caused by misregulation of steroid hormone receptors, like prostate or breast cancer To identify novel inhibitors for this immunophilin, we d...