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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14条记录   Pharmacophore Refinement Guides the Design of Nanomolar-Range Botulinum Neurotoxin Serotype A Light Chain Inhibitors [作者：NUSS JONATHAN E; DONG YUXIANG; WANNER LAURA M; RUTHEL GORDON; WIPF PETER; GUSSIO RICK; VENNERSTROM JONATHAN L; BAVARI SINA; BURNETT JAMES C,期刊：ACS Medicinal Chemistry Letters, 页码：301-305 , 文章类型： Article，,卷期：2010年1-7] Botulinum neurotoxins (BoNTs) are the deadliest of microbial toxins. The enzyme's zinc(II) metalloprotease, referred to as the light chain (LC) component, inhibits acetylcholine release into neuromuscular junctions, resu... Targeting the c-Kit Promoter G-quadruplexes with 6-Substituted Indenoisoquinolines [作者：BEJUGAM MALLESHAM; GUNARATNAM MEKALA; MUELLER SEBASTIAN; SANDERS DEBORAH A; SEWITZ SVEN; FLETCHER JONATHAN A; NEIDLE STEPHEN; BALASUBRAMANIAN SHANKAR,期刊：ACS Medicinal Chemistry Letters, 页码：306-310 , 文章类型： Article，,卷期：2010年1-7] Herein, we demonstrate the design, synthesis, biophysical properties, and preliminary biological evaluation of 6-substituted indenoisoquinolines as a new class of G-quadruplex stabilizing small molecule ligands. We have ... Synthesis and Evaluation of Noviose Replacements on Novobiocin That Manifest Antiproliferative Activity [作者：ZHAO HUIPING; KUSUMA BHASKAR REDDY; BLAGG BRIAN S J,期刊：ACS Medicinal Chemistry Letters, 页码：311-315 , 文章类型： Article，,卷期：2010年1-7] Structural modifications to the coumarin core and benzamide side chain of novobiocin have successfully transformed the natural product from a selective DNA gyrase inhibitor into a potent inhibitor of the Hsp90 C-terminus... Novel 3-Oxazolidinedione-6-aryl-pyridinones as Potent, Selective, and Orally Active EP3 Receptor Antagonists [作者：JIN JIAN; MORALESRAMOS ANGEL; EIDAM PATRICK; MECOM JOHN; LI YUE; BROOKS CARL; HILFIKER MARK; ZHANG DAVID; WANG NING; SHI DONGCHUAN; TSENG PEISAN; WHELESS KAREN; BUDZIK BRIAN; EVANS KAREN; JAWORSKI JONPAUL; JUGUS JACK; LEON LISA; WU CHARLENE; PULLEN MARK; KARAMSHI BHUMIKA; RAO PARVATHI; WARD EMMA; LAPING NICHOLAS; EVANS CHRISTOPHER; LEACH COLIN; HOLT DENNIS; SU XIN; MORROW DWIGHT; FRIES HARVEY; THORNELOE KEVIN; EDWARDS RICHARD,期刊：ACS Medicinal Chemistry Letters, 页码：316-320 , 文章类型： Article，,卷期：2010年1-7] High-throughput screening and subsequent optimization led to the discovery of novel 3-oxazolidinedione-6-aryl-pyridinones exemplified by compound 2 as potent and selective EP3-antagonists with excellent pharmacokinetic p... Fluorinated Benzofuran Derivatives for PET Imaging of beta-Amyloid Plaques in Alzheimer's Disease Brains [作者：CHENG YAN; ONO MASAHIRO; KIMURA HIROYUKI; KAGAWA SHINYA; NISHII RYUICHI; KAWASHIMA HIDEKAZU; SAJIO HIDEO,期刊：ACS Medicinal Chemistry Letters, 页码：321-325 , 文章类型： Article，,卷期：2010年1-7] A series of fluorinated benzofuran derivatives as potential tracers for positron emission tomography (PET) targeting beta-amyloid plaques in the brains of patients with Alzheimer's disease (AD) were synthesized and evalu... A Direct Comparison of the Anticancer Activities of Digitoxin MeON-Neoglycosides and O-Glycosides [作者：IYER ANAND KRISHNAN V; ZHOU MAOQUAN; AZAD NEELAM; ELBAZ HOSAM; WANG LEO; ROGALSKY DEREK K; ROJANASAKUL YON; ODOHERTY GEORGE A; LANGENHAN JOSEPH M,期刊：ACS Medicinal Chemistry Letters, 页码：326-330 , 文章类型： Article，,卷期：2010年1-7] Digitoxin is a cardiac glycoside currently being investigated for potential use in oncology; however, an investigation of anticancer activity as a function, of oligosaccharide chain length has not yet been performed. We ... Discovery of Potent and Selective Inhibitors of CDPK1 from C. parvum and T. gondii [作者：MURPHY RYAN C; OJO KAYODE K; LARSON ERIC T; CASTELLANOSGONZALEZ ALEJANDRO; PERERA B GAYANI K; KEYLOUN KATELYN R; KIM JESSICA E; BHANDARI JANHAVI G; MULLER NATASCHA R; VERLINDE CHRISTOPHE L M J; WHITE A CLINTON JR; MERRITT ETHAN A; VAN VOORHIS WESLEY C; MALY DUSTIN J,期刊：ACS Medicinal Chemistry Letters, 页码：331-335 , 文章类型： Article，,卷期：2010年1-7] The protozoans Cryptosporidium parvum and Toxoplasma gondii are parasites of major health concern to humans. Both parasites contain a group of calcium dependent protein kinases (CDPKs) which are found in plants and cilia... [Au-2(phen(2Me))(2)(mu-O)(2)](PF6)(2), a Novel Dinuclear Gold(III) Complex Showing Excellent Antiproliferative Properties [作者：CINELLU MARIA A; MAIORE LAURA; MANASSERO MARIO; CASINI ANGELA; ARCA MASSIMILIANO; FIEBIG HEINZHERBERT; KELTER GERHARD; MICHELUCCI ELENA; PIERACCINI GIUSEPPE; GABBIANI CHIARA; MESSORI LUIGI,期刊：ACS Medicinal Chemistry Letters, 页码：336-339 , 文章类型： Article，,卷期：2010年1-7] A novel dioxo-bridged dinuclear gold(III) complex with two 2,9-dimethylphenanthroline ligands was synthesized and thoroughly characterized. Its crystal structure was solved, and its solution behavior assessed. Remarkably... Novel and Potent 5-Piperazinyl Methyl-N-1-aryl Sulfonyl Indole Derivatives as 5-HT6 Receptor Ligands [作者：NIROGI RAMAKRISHNA V S; KOTHMIRKAR PRABHAKAR; KAMBHAMPATI RAMASASTRI; KONDA JAGADISH BABU; AREPALLI SOBHANADRI; PAMULETI NARASIMHAREDDY G; DESHPANDE AMOL D; BANDYALA TRINATHREDDY; SHINDE ANIL K; DUBEY P K,期刊：ACS Medicinal Chemistry Letters, 页码：340-344 , 文章类型： Article，,卷期：2010年1-7] The exclusive distribution of 5-HT6 receptors in the brain regions associated with learing and memory makes it an ideal target for cognitive disorders. A novel series of 5-piperazinyl methyl-N-1-aryl sulfonyl indoles wer... Structure-Activity Study of Dihydrocinnamic Acids and Discovery of the Potent FFA1 (GPR40) Agonist TUG-469 [作者：CHRISTIANSEN ELISABETH; DUEHANSEN MARIA E; URBAN CHRISTIAN; MERTEN NICOLE; PFLEIDERER MICHAEL; KARLSEN KASPER K; RASMUSSEN SANNE S; STEENSGAARD METTE; HAMACHER ALEXANDRA; SCHMIDT JOHANNES; DREWKE CHRISTEL; PETERSEN RASMUS KOEFOED; KRISTIANSEN KARSTEN; ULLRICH SUSANNE; KOSTENIS EVI; KASSACK MATTHIAS U; ULVEN TROND,期刊：ACS Medicinal Chemistry Letters, 页码：345-349 , 文章类型： Article，,卷期：2010年1-7] The free fatty acid 1 receptor (FFA1 or GPR40), which is highly expressed on pancreatic beta-cells and amplifies glucose-stimulated insulin secretion, has emerged as attractive target for the treatment of type 2 diabetes... Identification of an Orally Bioavailable, Potent, and Selective Inhibitor of GlyT1 [作者：BLACKABY WESLEY P; LEWIS RICHARD T; THOMSON JOANNE L; JENNINGS ANDREW S R; GOODACRE SIMON C; STREET LESLIE J; MACLEOD ANGUS M; PIKE ANDREW; WOOD SUZANNE; THOMAS STEVE; BROWN TERRY A; SMITH ALISON; PILLAI GOPALAN; ALMOND SARAH; GUSCOTT MARTIN R; BURNS H DONALD; ENG WAISI; RYAN CHRISTINE; COOK JACQUELYNN; HAMILL TERENCE G,期刊：ACS Medicinal Chemistry Letters, 页码：350-354 , 文章类型： Article，,卷期：2010年1-7] Amalgamation of the structure-activity relationship of two series of GlyT1 inhibitors developed at Merck led to the discovery of a clinical candidate, compound 16 (DCCCyB), which demonstrated excellent in vivo occupancy ... Identification and Characterization of Novel Inhibitors of mPTPB, an Essential Virulent Phosphatase from Mycobacterium tuberculosis [作者：CHEN LAN; ZHOU BO; ZHANG SHENG; WU LI; WANG YUEHONG; FRANZBLAU SCOTT G; ZHANG ZHONGYIN,期刊：ACS Medicinal Chemistry Letters, 页码：355-359 , 文章类型： Article，,卷期：2010年1-7] Mycobacterium protein tyrosine phosphatase B (mPTPB) is an essential virulence factor required for Mycobacterium tuberculosis (Mtb) survival in host macrophages. Consequently mPTPB represents an exciting new with a compl... Discovery of Novel Benzo[a]phenoxazine SSJ-183 as a Drug Candidate for Malaria [作者：GE JIANFENG; ARAI CHIKA; YANG MEI; MD ABU BAKAR; LU JUN; ISMAIL NASSER S M; WITTLIN SERGIO; KAISER MARCEL; BRUN RETO; CHARMAN SUSAN A; NGUYEN TIEN; MORIZZI JULIA; ITOH ISAMU; IHARA MASATAKA,期刊：ACS Medicinal Chemistry Letters, 页码：360-364 , 文章类型： Article，,卷期：2010年1-7] Malaria is a serious infectious disease caused by protozoan parasites in tropical and subtropical regions. Even inhabitants of temperate zones are exposed to the danger of malaria infection because of travel and global w... 1-Substituted 4-(3-Hydroxyphenyl)piperazines Are Pure Opioid Receptor Antagonists [作者：CARROLL F IVY; CUEVA JUAN PABLO; THOMAS JAMES B; MASCARELLA S WAYNE; RUNYON SCOTT P; NAVARRO HERNAN A,期刊：ACS Medicinal Chemistry Letters, 页码：365-369 , 文章类型： Article，,卷期：2010年1-7] This report describes the discovery that 1-substituted 4-(3-hydroxy-phenyl)piperazines are pure opioid receptor antagonists. Compounds in this new series include N-phenylpropyl (3S)-3-methyl-4-(3-hydroxyphenyl)piperazine...