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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49条记录   A Type-II Kinase Inhibitor Capable of Inhibiting the T315I "Gatekeeper" Mutant of Bcr-Abl [作者：CHOI HWAN GEUN; REN PINGDA; ADRIAN FRANCISCO; SUN FANGXIAN; LEE HYUN SOO; WANG XIA; DING QIANG; ZHANG GUOBAO; XIE YONGPING; ZHANG JIANMING; LIU YI; TUNTLAND TOVE; WARMUTH MARKUS; MANLEY PAUL W; MESTAN JUERGEN; GRAY NATHANAEL S; SIM TAEBO,期刊：Journal of Medicinal Chemistry, 页码：5439-5448 , 文章类型： Article，,卷期：2010年53-15] The second generation of Bcr-Abl inhibitors nilotinib, dasatinib, and bosutinib developed to override imatinib resistance are not active against the T315I "gatekeeper" mutation. Here we describe a type-II T315I inhibitor... Structural Optimization and Biological Evaluation of Substituted Bisphenol A Derivatives as beta-Amyloid Peptide Aggregation Inhibitors [作者：ZHOU YU; JIANG CHUNYI; ZHANG YAPING; LIANG ZHONGJIE; LIU WENFENG; WANG LIEFENG; LUO CHENG; ZHONG TINGTING; SUN YI; ZHAO LINXIANG; XIE XIN; JIANG HUALIANG; ZHOU NAIMING; LIU DONGXIANG; LIU HONG,期刊：Journal of Medicinal Chemistry, 页码：5449-5466 , 文章类型： Article，,卷期：2010年53-15] The aggregation of A beta is a crucial step in the etiology of Alzheimer's disease. Our previous work showed that A beta undergoes alpha-helix/beta-sheet intermediate structures during the conformational transition, and ... Phenylsulfonylfuroxans as Modulators of Multidrug-Resistance-Associated Protein-1 and P-Glycoprotein [作者：FRUTTERO ROBERTA; CROSETTI MARCO; CHEGAEV KONSTANTIN; GUGLIELMO STEFANO; GASCO ALBERTO; BERARDI FRANCESCO; NISO MAURO; PERRONE ROBERTO; PANARO MARIA ANTONIETTA; COLABUFO NICOLA ANTONIO,期刊：Journal of Medicinal Chemistry, 页码：5467-5475 , 文章类型： Article，,卷期：2010年53-15] A series of furoxan derivatives were studied for their ability to interact with P-gp and MRP1 transporters in MDCK cells overexpressing these proteins. 3-Phenylsulfonyl substituted furoxans emerged as the most interestin... Quinazolin-4-one Derivatives: A Novel Class of Noncompetitive NR2C/D Subunit-Selective N-Methyl-D-aspartate Receptor Antagonists [作者：MOSLEY CARA A; ACKER TIMOTHY M; HANSEN KASPER B; MULLASSERIL PRASEEDA; ANDERSEN KAREN T; LE PHUONG; VELLANO KIMBERLY M; BRAUNEROSBORNE HANS; LIOTTA DENNIS C; TRAYNELIS STEPHEN F,期刊：Journal of Medicinal Chemistry, 页码：5476-5490 , 文章类型： Article，,卷期：2010年53-15] We describe a new class of subunit-selective antagonists of N-methyl D-aspartate (NMDA)-selective ionotropic glutamate receptors that contain the (E)-3-phenyl-2-styrylquinazolin-4(3H)-one backbone. The inhibition of reco... Biological and Conformational Evaluation of Bifunctional Compounds for Opioid Receptor Agonists and Neurokinin 1 Receptor Antagonists Possessing Two Penicillamines [作者：YAMAMOTO TAKASHI; NAIR PADMA; JACOBSEN NEIL E; KULKARNI VINOD; DAVIS PEG; MA SHOUWU; NAVRATILOVA EDITA; YAMAMURA HENRY I; VANDERAH TODD W; PORRECA FRANK; LAI JOSEPHINE; HRUBY VICTOR J,期刊：Journal of Medicinal Chemistry, 页码：5491-5501 , 文章类型： Article，,卷期：2010年53-15] Neuropathic pain states and tolerance to opioids can result from system changes in the CNS, such as up-regulation of the NK1 receptor and substance P, lead to antiopioid effects in ascending or descending pain-signaling ... A Novel Water-Soluble Gossypol Derivative Increases Chemotherapeutic Sensitivity and Promotes Growth Inhibition in Colon Cancer [作者：YAN FEI; CAO XINGXIN; JIANG HAIXIA; ZHAO XIAOLONG; WANG JIANYONG; LIN YIHUI; LIU QIAOLING; ZHANG CHEN; JIANG BIAO; GUO FANG,期刊：Journal of Medicinal Chemistry, 页码：5502-5510 , 文章类型： Article，,卷期：2010年53-15] Compound 1 ((-)-gossypol) has been long known as a chemical anticancer agent. With its low water solubility and toxicity, it is not widely used as a commercial drug. To overcome these disadvantages, several novel derivat... Polyamines Inhibit Carbonic Anhydrases by Anchoring to the Zinc-Coordinated Water Molecule [作者：CARTA FABRIZIO; TEMPERINI CLAUDIA; INNOCENTI ALESSIO; SCOZZAFAVA ANDREA; KAILA KAI; SUPURAN CLAUDIU T,期刊：Journal of Medicinal Chemistry, 页码：5511-5522 , 文章类型： Article，,卷期：2010年53-15] Carbonic anhydrases (CAs, EC 4.2.1.1) are inhibited by sulfonamides, phenols, and coumarins. Polyamines such as spermine, spermidine, and many synthetic congeners are described to constitute a novel class of CA inhibitor... Identification of the First Low-Molecular-Weight Inhibitors of Matriptase-2 [作者：SISAY MIHIRET TEKESTE; STEINMETZER TORSTEN; STIRNBERG MARIT; MAURER EVA; HAMMAMI MAYA; BAJORATH JUERGEN; GUETSCHOW MICHAEL,期刊：Journal of Medicinal Chemistry, 页码：5523-5535 , 文章类型： Article，,卷期：2010年53-15] As recently discovered, matriptase-2, a type II transmembrane serine protease, plays a crucial role in body iron homeostasis by down-regulating hepcidin expression, which results in increased iron levels. Thus, matriptas... Development and Characterization of New Inhibitors of the Human and Mouse Hematopoietic Prostaglandin D-2 Synthases [作者：CHRIST ANGELIKA N; LABZIN LARISA; BOURNE GREGORY T; FUKUNISHI HIROTADA; WEBER JANE E; SWEET MATTHEW J; SMYTHE MARK L; FLANAGAN JACK U,期刊：Journal of Medicinal Chemistry, 页码：5536-5548 , 文章类型： Article，,卷期：2010年53-15] The hematopoietic prostaglandin D-2 synthase has a proinflammatory effect in a range of diseases, including allergic asthma, where its product prostaglandin D2 (PGD(2)) has a role in regulating many of the hallmark disea... Synthesis, Fluorine-18 Radiolabeling, and Biological Evaluation of N-((E)-4-Fluorobut-2-en-1-yl)-2 beta-carbomethoxy-3 beta-(4 '-halophenyl)nortropanes: Candidate Radioligands for In Vivo Imaging of the Brain Dopamine Transporter with Positron Emission Tomography [作者：STEHOUWER JEFFREY S; DANIEL LAURYN M; CHEN PING; VOLL RONALD J; WILLIAMS LARRY; PLOTT SUSAN J; VOTAW JOHN R; OWENS MICHAEL J; HOWELL LEONARD; GOODMAN MARK M,期刊：Journal of Medicinal Chemistry, 页码：5549-5557 , 文章类型： Article，,卷期：2010年53-15] The N-(E)-fluorobutenyl-3 beta-(para-halo-phenyl)nortropanes 9-12 were synthesized as ligands of the dopamine transporter (DAT) for use as F-18-labeled positron emission tomography (PET) imaging agents. In vitro competit... Unnatural Amino Acid Side Chains as S1, S1 ', and S2 ' Probes Yield Cationic Antimicrobial Peptides with Stability toward Chymotryptic Degradation [作者：KARSTAD RASMUS; ISAKSEN GEIR; BRANDSDAL BJORNOLAV; SVENDSEN JOHN SIGURD; SVENSON JOHAN,期刊：Journal of Medicinal Chemistry, 页码：5558-5566 , 文章类型： Article，,卷期：2010年53-15] This work describes how the systematic incorporation of a range of unnatural amino acid derivatives in the PI, P1', and P2' positions allows for the generation of short lactoferricin based cationic antimicrobial peptides... Substituted E-3-(3-Indolylmethylene)-1,3-dihydroindo1-2-ones with Antitumor Activity. In Depth Study of the Effect on Growth of Breast Cancer Cells [作者：ANDREANI ALDO; BELLINI STEFANIA; BURNELLI SILVIA; GRANAIOLA MASSIMILIANO; LEONI ALBERTO; LOCATELLI ALESSANDRA; MORIGI RITA; RAMBALDI MIRELLA; VAROLI LUCILLA; CALONGHI NATALIA; CAPPADONE CONCETTINA; ZINI MADDALENA; STEFANELLI CLAUDIO; MASOTTI LANFRANCO; SHOEMAKER ROBERT H,期刊：Journal of Medicinal Chemistry, 页码：5567-5575 , 文章类型： Article，,卷期：2010年53-15] The synthesis of new substituted E-3-(3-indolylmethylene)-1,3-dihydroindo1-2-ones is reported. The antitumor activity was evaluated according to protocols available at the National Cancer Institute (NCI), Bethesda, MD. S... Biological Diversity from a Structurally Diverse Library: Systematically Scanning Conformational Space Using a Pyranose Scaffold [作者：ABBENANTE GIOVANNI; BECKER BERND; BLANC SEBASTIEN; CLARK CHRIS; CONDIE GLENN; FRASER GRAEME; GRATHWOHL MATTHIAS; HALLIDAY JUDY; HENDERSON SENKA; LAM ANN; LIU LIGONG; MANN MARETTA; MULDOON CRAIG; PEARSON ANDREW; PREMRAJ RAJARATNAM; RAMSDALE TRADE; ROSSETTI TONY; SCHAFER KARL; LE THANH GIANG; TOMETZKI GERALD; VARI FRANK; VERQUIN GERALDINE; WAANDERS JENNIFER; WEST MICHAEL; WIMMER NORBERT; YAU ANNIKA; ZUEGG JOHANNES; MEUTERMANS WIM,期刊：Journal of Medicinal Chemistry, 页码：5576-5586 , 文章类型： Article，,卷期：2010年53-15] Success in discovering bioactive peptide mimetics is often limited by the difficulties in correctly transposing known binding elements of the active peptide onto a small and metabolically more stable scaffold while maint... Lysine N-epsilon-Trimethylation, a Tool for Improving the Selectivity of Antimicrobial Peptides [作者：FERNANDEZREYES MARIA; DIAZ DOLORES; DE LA TORRE BEATRIZ G; CABRALESRICO ANIA; VALLESMIRET MARIONA; JIMENEZBARBERO JESUS; ANDREU DAVID; RIVAS LUIS,期刊：Journal of Medicinal Chemistry, 页码：5587-5596 , 文章类型： Article，,卷期：2010年53-15] The effects of lysine N-epsilon-trimethylation at selected positions of the antimicrobial cecropin A melittin hybrid peptide KWKLFKKIGAVLKVL-amide have been studied. All five monotrimethylated, four bis-trimethylated plu... Computer-Aided Optimization of Phosphinic Inhibitors of Bacterial Ureases [作者：VASSILIOU STAMATIA; KOSIKOWSKA PAULINA; GRABOWIECKA AGNIESZKA; YIOTAKIS ATHANASIOS; KAFARSKI PAWEL; BERLICKI LUKASZ,期刊：Journal of Medicinal Chemistry, 页码：5597-5606 , 文章类型： Article，,卷期：2010年53-15] Urease inhibitors can be considered as a tool to control the damaging effect of ureolytic bacteria infections in humans which occur commonly in the developed countries. Computer-aided optimization of the aminomethylphosp... An Efficient Approach to the Discovery of Potent Inhibitors against Glycosyltransferases [作者：HOSOGUCHI KENSAKU; MAEDA TAKAHIRO; FURUKAWA JUNICHI; SHINOHARA YASURO; HINOU HIROSHI; SEKIGUCHI MITSUAKI; TOGAME HIROKO; TAKEMOTO HIROSHI; KONDO HIROSATO; NISHIMURA SHINICHIRO,期刊：Journal of Medicinal Chemistry, 页码：5607-5619 , 文章类型： Article，,卷期：2010年53-15] We describe a standardized approach for searching potent and selective inhibitors of glycosyltransferases by high throughput quantitative MALDI-TOFMS-based screening of focused compound libraries constructed by 1,3-dipol...