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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45条记录   Synthesis and SAR requirements of adamantane-colchicine conjugates with both microtubule depolymerizing and tubulin clustering activities [作者：ZEFIROVA OLGA N; NURIEVA EVGENIYA V; SHISHOV DMITRII V; BASKIN IGOR I; FUCHS FABIAN; LEMCKE HEIKO; SCHROEDER FABIAN; WEISS DIETER G; ZEFIROV NIKOLAY S; KUZNETSOV SERGEI A,期刊：Bioorganic & Medicinal Chemistry, 页码：5529-5538 , 文章类型： Article，,卷期：2011年19-18] A series of analogues of conjugate 1, combining an adamantane-based paclitaxel (taxol) mimetic with colchicine was synthesized and tested for cytotoxicity in a cell-based assay with the human lung carcinoma cell line A54... Discovery, synthesis, and structure-activity relationship of 6-aminomethyl-7,8-dihydronaphthalenes as human melanin-concentrating hormone receptor 1 antagonists [作者：KAMATA MAKOTO; YAMASHITA TOSHIRO; IMAEDA TOSHIHIRO; TANAKA TOSHIO; TERAUCHI JUN; MIYAMOTO MAKI; ORA TAIICHI; TAWADA MICHIKO; ENDO SATOSHI; TAKEKAWA SHIRO; ASAMI ASANO; SUZUKI NOBUHIRO; NAGISA YASUTAKA; NAKANO YOSHIHIDE; WATANABE KAORU; OGINO HITOMI; KATO KOKI; KATO KANEYOSHI; ISHIHARA YUJI,期刊：Bioorganic & Medicinal Chemistry, 页码：5539-5552 , 文章类型： Article，,卷期：2011年19-18] Human melanin-concentrating hormone receptor 1 (hMCHR1) antagonists are promising targets for obesity treatment. We identified the tetrahydronaphthalene derivative 1a with modest binding affinity for hMCHR1 by screening ... Synthesis and biological evaluation of HQCAs with aryl or benzyl substituents on N-1 position as potential HIV-1 integrase inhibitors [作者：HE QIUQIN; ZHANG XUAN; WU HAIQIU; GU SHUANGXI; MA XIAODONG; YANG LIUMENG; ZHENG YONGTANG; CHEN FENER,期刊：Bioorganic & Medicinal Chemistry, 页码：5553-5558 , 文章类型： Article，,卷期：2011年19-18] A series of new 5-hydroxylquinolone-3-carboxylic acids (HQCAs) with various aryl or benzyl substituents on N-1 position were synthesized and evaluated for their anti-HIV activity in C8166 cell culture. Most of the target... Inhibitory effects of chalcone glycosides isolated from Brassica rapa L. 'hidabeni' and their synthetic derivatives on LPS-induced NO production in microglia [作者：HARA HIROKAZU; NAKAMURA YOKO; NINOMIYA MASAYUKI; MOCHIZUKI RYOSUKE; KAMIYA TETSURO; AIZENMAN ELIAS; KOKETSU MAMORU; ADACHI TETSUO,期刊：Bioorganic & Medicinal Chemistry, 页码：5559-5568 , 文章类型： Article，,卷期：2011年19-18] Activation of microglia induces the production of various inflammatory mediators including nitric oxide (NO), leading to neurodegeneration in many central nervous system diseases. In this study, we examined the effects o... N-(1,3-Diaryl-3-oxopropyl)amides as a new template for xanthine oxidase inhibitors [作者：NEPALI KUNAL; AGARWAL AMIT; SAPRA SAMEER; MITTAL VINEET; KUMAR RAJ; BANERJEE UTTAM C; GUPTA MANISH K; SATTI NARESH K; SURI OM P; DHAR KANAYA L,期刊：Bioorganic & Medicinal Chemistry, 页码：5569-5576 , 文章类型： Article，,卷期：2011年19-18] A series of forty two N-(1,3-diaryl-3-oxopropyl)amides were synthesized via an efficient, modified Dakin-West reaction and were evaluated for in vitro xanthine oxidase inhibitory activity for the first time. Structure-ac... Synthesis and protective effects of aralkyl alcoholic 2-acetamido-2-deoxy-beta-D-pyranosides on hypoglycemia and serum limitation induced apoptosis in PC12 cell [作者：MENG YING; GUO YIBING; LING YONG; ZHAO YAHONG; ZHANG QI; ZHOU XINYANG; DING FEI; YANG YUMIN,期刊：Bioorganic & Medicinal Chemistry, 页码：5577-5584 , 文章类型： Article，,卷期：2011年19-18] Neuroprotective agents have been in the focus of attention in the treatment of ischemic stroke. Salidroside, a phenylpropanoid glycoside isolated from Rhodiola rosea L., possessed a wide range of biological activities, e... The structure-activity relationship of urea derivatives as anti-tuberculosis agents [作者：BROWN JOSHUA R; NORTH ELTON J; HURDLE JULIAN G; MORISSEAU CHRISTOPHE; SCARBOROUGH JERROD S; SUN DIANQING; KORDULAKOVA JANA; SCHERMAN MICHAEL S; JONES VICTORIA; GRZEGORZEWICZ ANNA; CREW REBECCA M; JACKSON MARY; MCNEIL MICHAEL R; LEE RICHARD E,期刊：Bioorganic & Medicinal Chemistry, 页码：5585-5595 , 文章类型： Article，,卷期：2011年19-18] The treatment of tuberculosis is becoming more difficult due to the ever increasing prevalence of drug resistance. Thus, it is imperative that novel anti-tuberculosis agents, with unique mechanisms of action, be discover... Design, synthesis, and biological evaluation of curcumin analogues as multifunctional agents for the treatment of Alzheimer's disease [作者：CHEN SHANGYING; CHEN YUAN; LI YANPING; CHEN SHUHAN; TAN JIAHENG; OU TIANMIAO; GU LIANQUAN; HUANG ZHISHU,期刊：Bioorganic & Medicinal Chemistry, 页码：5596-5604 , 文章类型： Article，,卷期：2011年19-18] A series of novel curcumin analogues were designed, synthesized, and evaluated as potential multifunctional agents for the treatment of AD. The in vitro studies showed that these compounds had better inhibitory propertie... Synthesis, structural, and biological evaluation of bis-heteroarylmaleimides and bis-heterofused imides [作者：FERRI NICOLA; RADICE TIZIANO; ANTONINO MANUELA; BECCALLI EGLE MARIA; TINELLI STELLA; ZUNINO FRANCO; CORSINI ALBERTO; PRATESI GRAZIELLA; RAGG ENZIO M; GELMI MARIA LUISA; CONTINI ALESSANDRO,期刊：Bioorganic & Medicinal Chemistry, 页码：5291-5299 , 文章类型： Article，,卷期：2011年19-18] Bis-2,3-heteroarylmaleimides and polyheterocondensed imides joined through nitrogen atoms of the N, N'-bis(ethyl)-1,3-propanediamine linker were prepared from substituted maleic anhydrides and symmetrical diamines in goo... Antifungal thiopeptide cyclothiazomycin B1 exhibits growth inhibition accompanying morphological changes via binding to fungal cell wall chitin [作者：MIZUHARA NAOKO; KURODA MANABU; OGITA AKIRA; TANAKA TOSHIO; USUKI YOSHINOSUKE; FUJITA KENICHI,期刊：Bioorganic & Medicinal Chemistry, 页码：5300-5310 , 文章类型： Article，,卷期：2011年19-18] Cyclothiazomycin B1 (CTB1) is an antifungal cyclic thiopeptide isolated from the culture broth of Streptomyces sp. HA 125-40. CTB1 inhibited the growth of several filamentous fungi including plant pathogens along with sw... Synthesis of benzo[3,4] azepino[1,2-b] isoquinolin-9-ones from 3-arylisoquinolines via ring closing metathesis and evaluation of topoisomerase I inhibitory activity, cytotoxicity and docking study [作者：HUE THI MY VAN; KHADKA DAULAT BIKRAM; YANG SU HUI; THANH NGUYEN LE; CHO SUK HEE; ZHAO CHAO; LEE IKSOO; KWON YOUNGJOO; LEE KYUNGTAE; KIM YONGCHUL; CHO WONJEA,期刊：Bioorganic & Medicinal Chemistry, 页码：5311-5320 , 文章类型： Article，,卷期：2011年19-18] Benzo[3,4] azepino[1,2-b] isoquinolinones were designed and developed as constraint forms of 3-arylisquinolines with an aim to inhibit topoisomerase I (topo I). Ring closing metathesis (RCM) of 3-arylisoquinolines with s... Chemical modifications of resveratrol for improved protein kinase C alpha activity [作者：DAS JOYDIP; PANY SATYABRATA; MAJHI ANJOY,期刊：Bioorganic & Medicinal Chemistry, 页码：5321-5333 , 文章类型： Article，,卷期：2011年19-18] Resveratrol (1) is a naturally occurring phytoalexin that affects a variety of human disease models, including cardio-and neuroprotection, immune regulation, and cancer chemoprevention. One of the possible mechanisms by ... 5a-Carba-beta-D-glucopyranose derivatives as novel sodium-dependent glucose cotransporter 2 (SGLT2) inhibitors for the treatment of type 2 diabetes [作者：OHTAKE YOSHIHITO; SATO TSUTOMU; MATSUOKA HIROHARU; NISHIMOTO MASAHIRO; TAKA NAOKI; TAKANO KOJI; YAMAMOTO KEISUKE; OHMORI MASAYUKI; HIGUCHI TAKASHI; MURAKATA MASATOSHI; KOBAYASHI TAKAMITSU; MORIKAWA KAZUMI; SHIMMA NOBUO; SUZUKI MASAYUKI; HAGITA HITOSHI; OZAWA KAZUHARU; YAMAGUCHI KOJI; KATO MOTOHIRO; IKEDA SACHIYA,期刊：Bioorganic & Medicinal Chemistry, 页码：5334-5341 , 文章类型： Article，,卷期：2011年19-18] 5a-Carba-beta-D-glucopyranose derivatives were synthesized and identified as novel SGLT2-selective inhibitors. These inhibitors exhibited potent SGLT2 inhibition with high selectivity over SGLT1. Among the tested compoun... Biochemical characterization of a novel type-II VEGFR2 kinase inhibitor: Comparison of binding to non-phosphorylated and phosphorylated VEGFR2 [作者：IWATA HIDEHISA; IMAMURA SHINICHI; HORI AKIRA; HIXON MARK S; KIMURA HIROYUKI; MIKI HIROSHI,期刊：Bioorganic & Medicinal Chemistry, 页码：5342-5351 , 文章类型： Article，,卷期：2011年19-18] A pyrrolo[3,2-d] pyrimidine-based type-II vascular endothelial growth factor receptor 2 ( VEGFR2) kinase inhibitor, compound 20d, displayed time-dependent inhibition of the non-phosphorylated catalytic domain of VEGFR2. ... Synthesis and biological evaluation of Matijing-Su derivatives as potent anti-HBV agents [作者：QIU JINGYING; XU BIXUE; HUANG ZHENGMING; PAN WEIDONG; CAO PEIXUE; LIU CHANGXIAO; HAO XIAOJIANG; SONG BAOAN; LIANG GUANGYI,期刊：Bioorganic & Medicinal Chemistry, 页码：5352-5360 , 文章类型： Article，,卷期：2011年19-18] A series of Matijing-Su (MTS, N-(N-benzoyl-L-phenylalanyl)-O-acetyl-L-phenylalanol) derivatives were synthesized and evaluated for their anti-hepatitis B virus (HBV) activity in 2.2.15 cells. The IC(50) of compounds 14a ... Design and synthesis of new prostaglandin D(2) receptor antagonists [作者：IWAHASHI MAKI; TAKAHASHI EIJI; TANAKA MOTOYUKI; MATSUNAGA YOKO; OKADA YUTAKA; MATSUMOTO RYOJI; NAMBU FUMIO; NAKAI HISAO; TODA MASAAKI,期刊：Bioorganic & Medicinal Chemistry, 页码：5361-5371 , 文章类型： Article，,卷期：2011年19-18] To identify new cost-effective prostaglandin D(2) (DP) receptor antagonists, a series of novel 3-benzoylaminophenylacetic acids were synthesized and biologically evaluated. Among those tested, some representative compoun...