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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   Discovery of a Potent Dihydrooxadiazole Series of Non-ATP-Competitive MK2 (MAPKAPK2) Inhibitors [作者：QIN JUN; DHONDI PAWAN; HUANG XIANHAI; ASLANIAN ROBERT; FOSSETTA JAMES; TIAN FANG; LUNDELL DANIEL; PALANI ANANDAN,期刊：ACS Medicinal Chemistry Letters, 页码：100-105 , 文章类型： Article，,卷期：2012年3-2] Inhibition of MK2 has been shown to offer advantages over that of p38 MAPK in the development of cures for inflammatory diseases such as arthritis. P38 MAPK knockout in mice was lethal, whereas MK2-null mice demonstrated... Discovery of PF-04449913, a Potent and Orally Bioavailable Inhibitor of Smoothened [作者：MUNCHHOF MICHAEL J; LI QIFANG; SHAVNYA ANDREI; BORZILLO GARY V; BOYDEN TRACEY L; JONES CHRISTOPHER S; LAGRECA SUSAN D; MARTINEZALSINA LUIS; PATEL NANDINI; PELLETIER KATHLEEN; REITER LARRY A; ROBBINS MICHAEL D; TKALCEVIC GEORGE T,期刊：ACS Medicinal Chemistry Letters, 页码：106-111 , 文章类型： Article，,卷期：2012年3-2] Inhibitors of the Hedgehog signaling pathway have generated a great deal of interest in the oncology area due to the mounting evidence of their potential to provide promising therapeutic options for patients. Herein, we ... Diversity-Oriented Synthesis Yields a Novel Lead for the Treatment of Malaria [作者：HEIDEBRECHT RICHARD W JR; MULROONEY CAROL; AUSTIN CHRISTOPHER P; BARKER ROBERT H JR; BEAUDOIN JENNIFER A; CHENG KEN CHIHCHIEN; COMER EAMON; DANDAPANI SIVARAMAN; DICK JUSTIN; DUVALL JEREMY R; EKLAND ERIC H; FIDOCK DAVID A; FITZGERALD MARK E; FOLEY MICHAEL; GUHA RAJARSHI; HINKSON PAUL; KRAMER MARTIN; LUKENS AMANDA K; MASI DANIELA; MARCAURELLE LISA A; SU XINZHUAN; THOMAS CRAIG J; WEIWER MICHEL; WIEGAND ROGER C; WIRTH DYANN; XIA MENGHANG; YUAN JING; ZHAO JINGHUA; PALMER MICHELLE; MUNOZ BENITO; SCHREIBER STUART,期刊：ACS Medicinal Chemistry Letters, 页码：112-117 , 文章类型： Article，,卷期：2012年3-2] Here, we describe the discovery of a novel antimalarial agent using phenotypic screening of Plasmodium falciparum asexual blood-stage parasites. Screening a novel compound collection created using diversity-oriented synt... Negamycin Analogue with Readthrough-Promoting Activity as a Potential Drug Candidate for Duchenne Muscular Dystrophy [作者：TAGUCHI AKIHIRO; NISHIGUCHI SHIGENOBU; SHIOZUKA MASATAKA; NOMOTO TAKAO; INA MAYUKO; NOJIMA SHOUTA; MATSUDA RYOICHI; NONOMURA YOSHIAKI; KISO YOSHIAKI; YAMAZAKI YURI; YAKUSHIJI FUMIKA; HAYASHI YOSHIO,期刊：ACS Medicinal Chemistry Letters, 页码：118-122 , 文章类型： Article，,卷期：2012年3-2] A series of (+)-negamycin 1 analogues were synthesized, and their readthrough-promoting activity was evaluated for nonsense mutations in Duchenne muscular dystrophy 3 (DMD). A structure activity relationship study indica... Discovery of a Novel Series of CHK1 Kinase Inhibitors with a Distinctive Hinge Binding Mode [作者：HUANG XIAOHUA; CHENG CLIFF C; FISCHMANN THIERRY O; DUCA JOSE S; YANG XIANSHU; RICHARDS MATTHEW; SHIPPS GERALD W JR,期刊：ACS Medicinal Chemistry Letters, 页码：123-128 , 文章类型： Article，,卷期：2012年3-2] A novel series of CHK1 inhibitors with a distinctive hinge binding mode, exemplified by 2-aryl-N-(2-(piperazin-1-yl)phenyl)thiazole-4-carboxamide, was discovered through high-throughput screening using the affinity selec... Discovery of Small Molecule Mer Kinase Inhibitors for the Treatment of Pediatric Acute Lymphoblastic Leukemia [作者：LIU JING; YANG CHAO; SIMPSON CATHERINE; DERYCKERE DEBORAH; VAN DEUSEN AMY; MILEY MICHAEL J; KIREEV DMITRI; NORRISDROUIN JACQUELINE; SATHER SUSAN; HUNTER DEBRA; KORBOUKH VICTORIA K; PATEL HARI S; JANZEN WILLIAM P; MACHIUS MISCHA; JOHNSON GARY L; EARP H SHELTON; GRAHAM DOUGLAS K; FRYE STEPHEN V; WANG XIAODONG,期刊：ACS Medicinal Chemistry Letters, 页码：129-134 , 文章类型： Article，,卷期：2012年3-2] Ectopic Mer expression promotes pro-survival signaling and contributes to leukemogenesis and chemoresistance in childhood acute lymphoblastic leukemia (ALL). Consequently, Mer kinase inhibitors may promote leukemic cell ... Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor [作者：HADDACH MUSTAPHA; MICHAUX JEROME; SCHWAEBE MICHAEL K; PIERRE FABRICE; OBRIEN SEAN E; BORSAN COSMIN; TRAN JOE; RAFFAELE NICHOLAS; RAVULA SUCHITRA; DRYGIN DENIS; SIDDIQUIJAIN ADAM; DARJANIA LEVAN; STANSFIELD RYAN; PROFFITT CHRIS; MACALINO DIWATA; STREINER NICOLE; BLIESATH JOSHUA; OMORI MAY; WHITTEN JEFFREY P; ANDERES KENNA; RICE WILLIAM G; RYCKMAN DAVID M,期刊：ACS Medicinal Chemistry Letters, 页码：135-139 , 文章类型： Article，,卷期：2012年3-2] Structure activity relationship analysis in a series of 3-(5-((2-oxoindolin-3-ylidene)methyl)furan-2-yl)amides identified compound 13, a pan-Pim kinases inhibitor with excellent biochemical potency and kinase selectivity... Discovery of GNF-5837, a Selective TRK Inhibitor with Efficacy in Rodent Cancer Tumor Models [作者：ALBAUGH PAM; FAN YI; MI YUAN; SUN FANGXIAN; ADRIAN FRANCISCO; LI NANXIN; JIA YONG; SARKISOVA YELENA; KREUSCH ANDREAS; HOOD TAMI; LU MIN; LIU GUOXUN; HUANG SHENLIN; LIU ZUOSHENG; LOREN JON; TUNTLAND TOVE; KARANEWSKY DONALD S; SEIDEL H MARTIN; MOLTENI VALENTINA,期刊：ACS Medicinal Chemistry Letters, 页码：140-145 , 文章类型： Article，,卷期：2012年3-2] Neurotrophins and their receptors (TRKs) play key roles in the development of the nervous system and the maintenance of the neural network. Accumulating evidence points to their role in malignant transformations, chemota... Small Molecule Inhibitors of Regulators of G Protein Signaling (RGS) Proteins [作者：TURNER EMMA M; BLAZER LEVI L; NEUBIG RICHARD R; HUSBANDS STEPHEN M,期刊：ACS Medicinal Chemistry Letters, 页码：146-150 , 文章类型： Article，,卷期：2012年3-2] Recently, regulators of G protein signaling (RGS) proteins have emerged as potential therapeutic targets since they provide an alternative method of modulating the activity of G protein-coupled receptors, the target of s... Heteroaromatic Moieties in the Sphingosine Backbone of alpha-Galactosylceramides for Noncovalent Interactions with CD1d [作者：KIM YONGJU; KIM JONGHOON; OH KEUNHEE; LEE DONGSUP; PARK SEUNG BUM,期刊：ACS Medicinal Chemistry Letters, 页码：151-154 , 文章类型： Article，,卷期：2012年3-2] A series of alpha-GalCer analogues containing heterocyclic and aromatic moieties in the sphingosine backbone were synthesized to improve the selectivity in the Th1/Th2 cytokine profile via noncovalent interaction with th... Dual-Target Virtual Screening by Pharmacophore Elucidation and Molecular Shape Filtering [作者：MOSER DANIEL; WISNIEWSKA JOANNA M; HAHN STEFFEN; ACHENBACH JANOSCH; BUSCATO ESTELLA; KLINGLER FRANCAMARIA; HOFMANN BETTINA; STEINHILBER DIETER; PROSCHAK EWGENIJ,期刊：ACS Medicinal Chemistry Letters, 页码：155-158 , 文章类型： Article，,卷期：2012年3-2] Dual-target inhibitors gained increased attention in the past years. A novel in silico approach was employed for the discovery of dual 5-lipoxygenase/soluble epoxide hydrolase inhibitors. The ligand-based approach uses e... Virtual Screening and X-ray Crystallography for Human Kallikrein 6 Inhibitors with an Amidinothiophene P1 Group [作者：LIANG GUYAN; CHEN XIN; ALDOUS SUZANNE; PU SUFEN; MEHDI SHUJAATH; POWERS ELAINE; GIOVANNI ANDREW; KONGSAMUT SATHAPANA; XIA TIANHUI; ZHANG YING; WANG RACHEL; GAO ZHONGLI; MERRIMAN GREGORY; MCLEAN LARRY R; MORIZE ISABELLE,期刊：ACS Medicinal Chemistry Letters, 页码：159-164 , 文章类型： Article，,卷期：2012年3-2] A series of compounds with an amidinothiophene P1 group and a pyrrolidinone-sulphonamide scaffold linker was identified as potent inhibitors of human kallikrein 6 by structure-based virtual screening based on the union a... Discovery of Natural Phenols as G Protein-Coupled Receptor-35 (GPR35) Agonists [作者：DENG HUAYUN; HU HAIBEI; LING SHIZHANG; FERRIE ANN M; FANG YE,期刊：ACS Medicinal Chemistry Letters, 页码：165-169 , 文章类型： Article，,卷期：2012年3-2] We report the discovery and characterization of natural phenols as G protein-coupled receptor-35 (GPR35) agonists. Pharmacological characterization using label-free dynamic mass redistribution and Tango beta-arrestin tra... Highly Selective and Potent Thiophenes as PI3K Inhibitors with Oral Antitumor Activity. (vol 2, pg 809, 2011) [作者：LIU KEVIN KC; ZHU JINJIANG; SMITH GRAHAM L; YIN MINJEAN; BAILEY SIMON; CHEN JEFFREY H; HU QIYUE; HUANG QINHUA; LI CHUNZE; LI QING J; MARX MATTHEW A; PADERES GENEVIEVE; RICHARDSON PAUL F; SACH NEAL W; WALLS MARLENA; WELLS PETER A; BAXI SANGITA; ZOU AIHUA,期刊：ACS Medicinal Chemistry Letters, 页码：170-170 , 文章类型： Correction，,卷期：2012年3-2] Future Horizons in Drug Discovery Research [作者：REITZ ALLEN B,期刊：ACS Medicinal Chemistry Letters, 页码：80-82 , 文章类型： Editorial Material，,卷期：2012年3-2] Potentiating Metronidazole Scaffold against Resistant Trichomonas: Design, Synthesis, Biology and 3D-QSAR Analysis [作者：KUMAR LALIT; JAIN ASHISH; LAL NAND; SARSWAT AMIT; JANGIR SANTOSH; KUMAR LOKESH; SINGH VISHAL; SHAH PRIYANKA; JAIN SWATANTRA K; MAIKHURI JAGDAMBA P; SIDDIQI MOHAMMAD I; GUPTA GOPAL; SHARMA VISHNU L,期刊：ACS Medicinal Chemistry Letters, 页码：83-87 , 文章类型： Article，,卷期：2012年3-2] Metronidazole (MTZ), the FDA-approved drug against Trichomonas vaginalis (TV), is being challenged seriously by drug resistance, while its inertness to sperm makes it ineffective as a vaginal contraceptive. Thirteen pipe...