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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48条记录   Structure-based design of rhodanine-based acylsulfonamide derivatives as antagonists of the anti-apoptotic Bcl-2 protein [作者：LI HUANQIU; YANG JING; MA SHUHUA; QIAO CHUNHUA,期刊：Bioorganic & Medicinal Chemistry, 页码：4194-4200 , 文章类型： Article，,卷期：2012年20-14] A series of novel rhodanine-based acylsulfonamide derivatives were designed, synthesized, and evaluated as small-molecule inhibitors of anti-apoptotic Bcl-2 protein. These compounds exhibit potent antiproliferative activ... Novel retinoic acid 4-hydroxylase (CYP26) inhibitors based on a 3-(1H-imidazol- and triazol-1-yl)-2,2-dimethyl-3-(4-(phenylamino)phenyl)propyl scaffold [作者：GOMAA MOHAMED S; BRIDGENS CAROLINE E; ILLINGWORTH NICOLA A; VEAL GARETH J; REDFERN CHRISTOPHER P F; BRANCALE ANDREA; ARMSTRONG JANE L; SIMONS CLAIRE,期刊：Bioorganic & Medicinal Chemistry, 页码：4201-4207 , 文章类型： Article，,卷期：2012年20-14] Retinoic acid (RA), the biologically active metabolite of vitamin A, is used medicinally for the treatment of hyperproliferative diseases including dermatological conditions and cancer. The antiproliferative effects of R... Design, synthesis and biological activity of 6-substituted carbamoyl benzimidazoles as new nonpeptidic angiotensin II AT(1) receptor antagonists [作者：ZHANG JUN; WANG JINLIANG; ZHOU ZHIMING; LI ZHIHUAI; XUE WEIZHE; XU DI; HAO LIPING; HAN XIAOFENG; FEI FAN; LIU TING; LIANG AIHUA,期刊：Bioorganic & Medicinal Chemistry, 页码：4208-4216 , 文章类型： Article，,卷期：2012年20-14] A series of 6-substituted carbamoyl benzimidazoles were designed and synthesised as new nonpeptidic angiotensin II AT(1) receptor antagonists. The preliminary pharmacological evaluation revealed a nanomolar AT(1) recepto... Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents [作者：GANGJEE ALEEM; ZHAO YING; IHNAT MICHAEL A; THORPE JESSICA E; BAILEYDOWNS LORA C; KISLIUK ROY L,期刊：Bioorganic & Medicinal Chemistry, 页码：4217-4225 , 文章类型： Article，,卷期：2012年20-14] We designed, synthesized and evaluated 13 novel tricyclic indeno[2,1-d]pyrimidines as RTK inhibitors. These analogues were synthesized via a Dieckmann condensation of 1,2-phenylenediacetonitrile followed by cyclocondensa... Design, synthesis, biological evaluation and molecular modeling of novel 1,3,4-oxadiazole derivatives based on Vanillic acid as potential immunosuppressive agents [作者：TANG JIANFENG; LV XIANHAI; WANG XIAOLIANG; SUN JIAN; ZHANG YANBIN; YANG YUSHUN; GONG HAIBIN; ZHU HAILIANG,期刊：Bioorganic & Medicinal Chemistry, 页码：4226-4236 , 文章类型： Article，,卷期：2012年20-14] In present study, a series of novel 1,3,4-oxadiazole derivatives have been designed, synthesized and purified. All of these compounds are reported for the first time, the chemical structures of these compounds were confi... Novel 5-substituted benzyloxy-2-arylbenzofuran-3-carboxylic acids as calcium activated chloride channel inhibitors [作者：KUMAR SATISH; NAMKUNG WAN; VERKMAN A S; SHARMA PAWAN K,期刊：Bioorganic & Medicinal Chemistry, 页码：4237-4244 , 文章类型： Article，,卷期：2012年20-14] Transmembrane protein 16A (TMEM16A) channels are recently discovered membrane proteins that functions as a calcium activated chloride channel (CaCC). CaCCs are major regulators of various physiological processes, such as... Synthesis and SAR-study for novel arylpiperazine derivatives of 5-arylidenehydantoin with alpha(1)-adrenoceptor antagonistic properties [作者：HANDZLIK JADWIGA; SZYMANSKA EWA; WOJCIK RENATA; DELA ANNA; JASTRZEBSKAWIESEK MAGDALENA; KAROLAKWOJCIECHOWSKA JANINA; FRUZINSKI ANDRZEJ; SIWEK AGATA; FILIPEK BARBARA; KIECKONONOWICZ KATARZYNA,期刊：Bioorganic & Medicinal Chemistry, 页码：4245-4257 , 文章类型： Article，,卷期：2012年20-14] The study is focused on a series of 5-arylidenehydantoin derivatives with a phenylpiperazine-hydroxypropyl fragment at N3 of the hydantoin ring. The compounds were assessed on their affinity for alpha(1)-adrenoceptors an... Selective hydroboration of dieneamines. Formation of hydroxyalkylphenothiazines as MDR modulators [作者：TAKACS DANIELLA; NAGY ILDIKO; BOMBICZ PETRA; EGYED ORSOLYA; JEMNITZ KATALIN; RIEDL ZSUZSANNA; MOLNAR JOZSEF; AMARAL LEONARD; HAJOS GYOERGY,期刊：Bioorganic & Medicinal Chemistry, 页码：4258-4270 , 文章类型： Article，,卷期：2012年20-14] N-dienylphenothiazines synthesized from tetrazolo[1,5-a]pyridinium salts by treatment with phenothiazine were subjected to catalytic hydrogenation to yield N-butylphenothiazines, whereas transformation of these dienes wi... Synthesis and biological evaluation of novel anticancer bivalent colchicine-tubulizine hybrids [作者：MALYSHEVA YULIA B; COMBES SEBASTIEN; ALLEGRO DIANE; PEYROT VINCENT; KNOCHEL PAUL; GAVRYUSHIN ANDREI E; FEDOROV ALEXEY YU,期刊：Bioorganic & Medicinal Chemistry, 页码：4271-4278 , 文章类型： Article，,卷期：2012年20-14] A series of novel antimitotic hybrids were synthesized in good yields by linking of azide-containing colchicine congeners with acetylene-substituted tubulizine-type derivatives using copper-mediated 1,3-dipolar cycloaddi... Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents [作者：YAMAZAKI YURI; SUMIKURA MAKIKO; MASUDA YURIKA; HAYASHI YOSHIKI; YASUI HIROYUKI; KISO YOSHIAKI; CHINEN TAKUMI; USUI TAKEO; YAKUSHIJI FUMIKA; POTTS BARBARA; NEUTEBOOM SASKIA; PALLADINO MICHAEL; LLOYD GEORGE KENNETH; HAYASHI YOSHIO,期刊：Bioorganic & Medicinal Chemistry, 页码：4279-4289 , 文章类型： Article，,卷期：2012年20-14] KPU-105 (4), a potent anti-microtubule agent that contains a benzophenone was derived from the dike-topiperazine-type vascular disrupting agent (VDA) plinabulin 3, which displays colchicine-like tubulin depolymerization ... Thiorhodamines containing amide and thioamide functionality as inhibitors of the ATP-binding cassette drug transporter P-glycoprotein (ABCB1) [作者：ORCHARD ALEXANDRA; SCHAMERHORN GREGORY A; CALITREE BRANDON D; SAWADA GERI A; LOO TIP W; BARTLETT M CLAIRE; CLARKE DAVID M; DETTY MICHAEL R,期刊：Bioorganic & Medicinal Chemistry, 页码：4290-4302 , 文章类型： Article，,卷期：2012年20-14] Twelve thiorhodamine derivatives have been examined for their ability to stimulate the ATPase activity of purified human P-glycoprotein (P-gp)-His(10), to promote uptake of calcein AM and vinblastine into multidrug-resis... Bisubstrate analog inhibitors of 6-hydroxymethyl-7,8-dihydropterin pyrophosphokinase: New lead exhibits a distinct binding mode [作者：SHI GENBIN; SHAW GARY; LI YUE; WU YAN; YAN HONGGAO; JI XINHUA,期刊：Bioorganic & Medicinal Chemistry, 页码：4303-4309 , 文章类型： Article，,卷期：2012年20-14] 6-Hydroxymethyl-7,8-dihydropterin pyrophosphokinase (HPPK), a key enzyme in the folate biosynthesis pathway catalyzing the pyrophosphoryl transfer from ATP to 6-hydroxymethyl-7,8-dihydropterin, is an attractive target fo... Quencher-free molecular beacon tethering 7-hydroxycoumarin detects targets through protonation/deprotonation [作者：KASHIDA HIROMU; YAMAGUCHI KYOHEI; HARA YUICHI; ASANUMA HIROYUKI,期刊：Bioorganic & Medicinal Chemistry, 页码：4310-4315 , 文章类型： Article，,卷期：2012年20-14] In this study, we synthesized a simple but efficient quencher-free molecular beacon tethering 7-hydroxycoumarin on D-threoninol based on its pK(a) change. The pK(a) of 7-hydroxycoumarin in a single strand was determined ... Design, synthesis and antimicrobial activities of nitroimidazole derivatives containing 1,3,4-oxadiazole scaffold as FabH inhibitors [作者：LI YAO; LUO YIN; HU YANG; ZHU DIDI; ZHANG SHUAI; LIU ZHIJUN; GONG HAIBIN; ZHU HAILIANG,期刊：Bioorganic & Medicinal Chemistry, 页码：4316-4322 , 文章类型： Article，,卷期：2012年20-14] Nitroimidazoles and their derivatives have drawn continuing interest over the years because of their varied biological activities, recently found application in drug development for antimicrobial chemotherapeutics and an... Design, synthesis and antitumor activities of novel bis-aryl ureas derivatives as Raf kinase inhibitors [作者：ZHAN WENHU; LI YANYANG; HUANG WEIPING; ZHAO YANJIN; YAO ZHENGLIN; YU SHANYOU; YUAN SHOUJUN; JIANG FALONG; YAO SHAN; LI SHUXIN,期刊：Bioorganic & Medicinal Chemistry, 页码：4323-4329 , 文章类型： Article，,卷期：2012年20-14] A series of novel bis-aryl ureas containing trifluoromethyl imidazolyl group targeting Raf kinase were designed and synthesized based on the lead compound of Sorafenib. All the prepared compounds were evaluated for their... Synthesis and evaluation of a radioiodinated bladder cancer specific peptide [作者：HA YEONG SU; LEE HWA YOUNG; IL AN GWANG; KIM JONGHEE; KWAK WONJUNG; LEE EUNJU; LEE SEUNGMIN; LEE BYUNGHEON; KIM INSAN; BELAY TAKELE; LEE WOONGHEE; AHN BYEONGCHEOL; LEE JAETAE; YOO JEONGSOO,期刊：Bioorganic & Medicinal Chemistry, 页码：4330-4335 , 文章类型： Article，,卷期：2012年20-14] Bladder cancer is the second most common cancer of the urinary tract, however the invasive cystoscopy is still the standard technique for diagnosis and surveillance of bladder cancer. Herein, we radiolabel bladder cancer...