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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24条记录   Novel diarylpyridinones, diarylpyridazinones and diarylphthalazinones as potential HIV-1 nonnucleoside reverse transcriptase inhibitors (NNRTIs) [作者：VENKATRAJ MUTHUSAMY; ARIEN KEVIN K; HEERES JAN; DIRIE BERTRAND; JOOSSENS JURGEN; VAN GOETHEM SEBASTIAAN; VAN DER VEKEN PIETER; MICHIELS JOHAN; VELDE CHRISTOPHE M L VANDE; VANHAM GUIDO; LEWI PAW J; AUGUSTYNS KOEN,期刊：Bioorganic & Medicinal Chemistry, 页码：5924-5934 , 文章类型： Article，,卷期：2011年19-20] In this Letter, we report on diarylpyridinone, diarylpyridazinone and diarylphthalazinone analogs as potential inhibitors of HIV-1 nonnucleoside reverse transcriptase (NNRTIs). The most promising compounds in these serie... Structure-based design of dipeptide derivatives for the human neutral endopeptidase [作者：MISAWA KENSUKE; SUZUKI YASUTO; TAKAHASHI SATOSHI; YOSHIMORI ATSUSHI; TAKASAWA RYOKO; SHIBUYA YUSUKE; TANUMA SEIICHI,期刊：Bioorganic & Medicinal Chemistry, 页码：5935-5947 , 文章类型： Article，,卷期：2011年19-20] Neutral endopeptidase (NEP) plays a key role in the metabolic inactivation of various bioactive peptides such as atrial natriuretic peptide (ANP), endothelins, and enkephalins. Furthermore, NEP is known to work as elasta... Synthesis and antitumor activity of 1,2,4-triazoles having 1,4-benzodioxan fragment as a novel class of potent methionine aminopeptidase type II inhibitors [作者：HOU YAPING; SUN JUAN; PANG ZHONGHUA; LV PENGCHENG; LI DONGDONG; YAN LI; ZHANG HONGJIA; ZHENG EMILY XI; ZHAO JING; ZHU HAILIANG,期刊：Bioorganic & Medicinal Chemistry, 页码：5948-5954 , 文章类型： Article，,卷期：2011年19-20] A series of 1,2,4-triazole derivatives containing 1,4-benzodioxan (5a-5q) have been designed, synthesized, structurally determined, and their biological activities were evaluated as potential MetAP2 inhibitors. All the s... Pyrazolo[1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines and their tricyclic derivatives as corticotropin-releasing factor 1 (CRF(1)) receptor antagonists [作者：SAITO TETSUJI; OBITSU TETSUO; MINAMOTO CHIAKI; SUGIURA TSUNEYUKI; MATSUMURA NAOYA; UENO SONOKO; KISHI AKIHIRO; KATSUMATA SEISHI; NAKAI HISAO; TODA MASAAKI,期刊：Bioorganic & Medicinal Chemistry, 页码：5955-5966 , 文章类型： Article，,卷期：2011年19-20] To identify structurally novel CRF1 receptor antagonists, a series of bicyclic core antagonists, pyrazolo [1,5-a]pyrimidines, triazolo[1,5-a]pyrimidines, imidazo[1,2-a]pyrimidines and pyrazolo[1,5-a][1,3,5]triazines were... Solid-state NMR analysis of interaction sites of curcumin and 42-residue amyloid beta-protein fibrils [作者：MASUDA YUICHI; FUKUCHI MASASHI; YATAGAWA TATSUYA; TADA MASATO; TAKEDA KAZUYUKI; IRIE KAZUHIRO; AKAGI KENICHI; MONOBE YOUKO; IMAZAWA TAKAYOSHI; TAKEGOSHI K,期刊：Bioorganic & Medicinal Chemistry, 页码：5967-5974 , 文章类型： Article，,卷期：2011年19-20] Aggregation of 42-residue amyloid beta-protein (A beta 42) plays a pivotal role in the etiology of Alzheimer's disease (AD). Curcumin, the yellow pigment in the rhizome of turmeric, attracts considerable attention as a f... Potent inhibition of Norwalk virus by cyclic sulfamide derivatives [作者：DOU DENGFENG; TIEW KOKCHUAN; HE GUIJIA; MANDADAPU SIVAKOTESWARA RAO; ARAVAPALLI SRIDHAR; ALLISTON KEVIN R; KIM YUNJEONG; CHANG KYEONGOK; GROUTAS WILLIAM C,期刊：Bioorganic & Medicinal Chemistry, 页码：5975-5983 , 文章类型： Article，,卷期：2011年19-20] A new class of compounds that exhibit anti-norovirus activity in a cell-based system and embody in their structure a cyclosulfamide scaffold has been identified. The structure of the initial hit (compound 2a, ED(50) 4 mu... Synthesis of a series of 3,4-methanoarginines as side-chain conformationally restricted analogues of arginine [作者：WATANABE MIZUKI; YAMAGUCHI KAZUYA; TANG WEI; YOSHIDA KEISUKE; SILVERMAN RICHARD B; ARISAWA MITSUHIRO; SHUTO SATOSHI,期刊：Bioorganic & Medicinal Chemistry, 页码：5984-5988 , 文章类型： Article，,卷期：2011年19-20] A series of optically active stereoisomers of 3,4-methanoarginine (1-4 and ent-1-ent-4) with trans/cis, D/L, and syn/anti stereochemical diversity, the side-chains of which were restricted in various special arrangements... The effect of a bromide leaving group on the properties of nitro analogs of the duocarmycins as hypoxia-activated prodrugs and phosphate pre-prodrugs for antitumor therapy [作者：STEVENSON RALPH J; DENNY WILLIAM A; ASHOORZADEH AMIR; PRUIJN FREDERIK B; VAN LEEUWEN WOUTER F; TERCEL MOANA,期刊：Bioorganic & Medicinal Chemistry, 页码：5989-5998 , 文章类型： Article，,卷期：2011年19-20] Nitro seco analogs (nitroCBIs) of the antitumor antibiotic duocarmycins are a new class of hypoxia activated prodrugs. These compounds undergo hypoxia-selective metabolism to form potent DNA alkylating agents. A series o... Inhibition of steroid sulfatase with 4-substituted estrone and estradiol derivatives [作者：CHAUMINH PHAN; LIU YONG; KIM BYOUNGMOO; MOSTAFA YASER; TAYLOR SCOTT D,期刊：Bioorganic & Medicinal Chemistry, 页码：5999-6005 , 文章类型： Article，,卷期：2011年19-20] Steroid sulfatase (STS) catalyzes the desulfation of biologically inactive sulfated steroids to yield biologically active desulfated steroids and is currently being examined as a target for therapeutic intervention for t... Synthesis and biological evaluation of a novel class of isatin analogs as dual inhibitors of tubulin polymerization and Akt pathway [作者：KRISHNEGOWDA GOWDAHALLI; GOWDA A S PRAKASHA; TAGARAM HEPHZIBAH RANI S; CARROLL KEVIN F STAVELEYO; IRBY ROSALYN B; SHARMA ARUN K; AMIN SHANTU,期刊：Bioorganic & Medicinal Chemistry, 页码：6006-6014 , 文章类型： Article，,卷期：2011年19-20] A novel series of 5,7-dibromoisatin analogs were synthesized and evaluated for their cytotoxicities against four human cancer cell lines including colon HT29, breast MCF-7, lung A549 and melanoma UACC903. Analogs 6, 11 a... Design, synthesis and biological evaluation of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as aminopeptidase N/CD13 inhibitors [作者：ZHANG XIAOPAN; ZHANG JIAN; ZHANG LEI; FENG JINGHONG; XU YINGYING; YUAN YUMEI; FANG HAO; XU WENFANG,期刊：Bioorganic & Medicinal Chemistry, 页码：6015-6025 , 文章类型： Article，,卷期：2011年19-20] A series of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed, synthesized and assayed for their activities against aminopeptidase N (APN/CD13) and MMP-2. The results showed that most compo... The discovery of long-acting saligenin beta(2) adrenergic receptor agonists incorporating a urea group [作者：PROCOPIOU PANAYIOTIS A; BARRETT VICTORIA J; FORD ALISON J; LOOKER BRIAN E; LUNNISS GILLIAN E; NEEDHAM DEBORAH; SMITH CLAIRE E; SOMERS GRAHAM,期刊：Bioorganic & Medicinal Chemistry, 页码：6026-6032 , 文章类型： Article，,卷期：2011年19-20] A series of novel, potent and selective human beta(2) adrenoceptor agonists incorporating a urea moiety on the terminal right-hand side phenyl ring of (R)-salmeterol is presented. Urea 9j had long duration of action in v... Anti-obesity effects of the methanolic extract and chakasaponins from the flower buds of Camellia sinensis in mice [作者：HAMAO MAKOTO; MATSUDA HISASHI; NAKAMURA SEIKOU; NAKASHIMA SOUICHI; SEMURA SHUNSUKE; MAEKUBO SAORI; WAKASUGI SACHIYO; YOSHIKAWA MASAYUKI,期刊：Bioorganic & Medicinal Chemistry, 页码：6033-6041 , 文章类型： Article，,卷期：2011年19-20] The methanolic extract from the flower buds of Camellia sinensis cultivated in Fujian Province showed inhibitory effects on body weight gain and the weight of visceral fats in high-fat diet-fed mice and/or Tsumura Suzuki... Synthesis and biological evaluation of phenstatin metabolites [作者：GHINET ALINA; RIGO BENOIT; HENICHART JEANPIERRE; LE BROCRYCKEWAERT DELPHINE; POMMERY JEAN; POMMERY NICOLE; THURU XAVIER; QUESNEL BRUNO; GAUTRET PHILIPPE,期刊：Bioorganic & Medicinal Chemistry, 页码：6042-6054 , 文章类型： Article，,卷期：2011年19-20] Previous investigations on the incubation of phenstatin with rat and human microsomal fractions revealed the formation of nine main metabolites. The structures of eight of these metabolites have been now confirmed by syn... Lead identification of beta-lactam and related imine inhibitors of the molecular chaperone heat shock protein 90 [作者：OBOYLE NIAMH M; KNOX ANDREW J S; PRICE TREVOR T; WILLIAMS D CLIVE; ZISTERER DANIELA M; LLOYD DAVID G; MEEGAN MARY J,期刊：Bioorganic & Medicinal Chemistry, 页码：6055-6068 , 文章类型： Article，,卷期：2011年19-20] Heat shock protein 90 is an emerging target for oncology therapeutics. Inhibitors of this molecular chaperone, which is responsible for the maintenance of a number of oncogenic proteins, have shown promise in clinical tr... Metronidazole acid acyl sulfonamide: A novel class of anticancer agents and potential EGFR tyrosine kinase inhibitors [作者：LUO YIN; LI YAO; QIU KEMING; LU XIANG; FU JIE; ZHU HAILIANG,期刊：Bioorganic & Medicinal Chemistry, 页码：6069-6076 , 文章类型： Article，,卷期：2011年19-20] A series of novel metronidazole derivatives were recently reported as potent anticancer agents targeting EGFR and HER-2 by our group [Qian, Y.; Zhang, H. J.; Zhang, H.; Xu, C.; Zhao, J.; Zhu, H. L Bioorg. Med. Chem. 2010...