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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28条记录   Conformationally Constrained Analogues of Diacylglycerol. 29. Cells Sort Diacylglycerol-Lactone Chemical Zip Codes to Produce Diverse and Selective Biological Activities. [作者：Duan, Dehui;Sigano, Dina M.;Kelley, James A.;Lai, Christopher C.;Lewin, Nancy E.;Kedei, Noemi;Peach, Megan L.;Lee, Jeewoo;Abeyweera, Thushara P.;Rotenberg, Susan A.;Kim, Hee;Kim, Young Ho;El Kazzouli, Said;Chung, Jae-Uk;Young, Howard A.;Young, Matthew R.;,期刊：Journal of Medicinal Chemistry, 页码：5198-5220 , 文章类型： 研究论文，,卷期：2008年51-17] Diacylglycerol-lactone (DAG-lactone) libraries generated by a solid-phase approach using IRORI technol. produced a variety of unique biol. activities. Subtle differences in chem. diversity in two areas of the mol., the ... Synthesis of Novel b-Lactone Inhibitors of Fatty Acid Synthase. [作者：Richardson, Robyn D.;Ma, Gil;Oyola, Yatsandra;Zancanella, Manuel;Knowles, Lynn M.;Cieplak, Piotr;Romo, Daniel;Smith, Jeffrey W.;,期刊：Journal of Medicinal Chemistry, 页码：5285-5296 , 文章类型： 研究论文，,卷期：2008年51-17] (Heterocyclic Compounds (One Hetero Atom)) Section Fatty acid synthase (FAS) is necessary for growth and survival of tumor cells and is a promising drug target for oncol. Here, we report on the syntheses and activity of... Roscovitine-Derived, Dual-Specificity Inhibitors of Cyclin-Dependent Kinases and Casein Kinases 1. [作者：Oumata, Nassima;Bettayeb, Karima;Ferandin, Yoan;Demange, Luc;Lopez-Giral, Angela;Goddard, Marie-Lorene;Myrianthopoulos, Vassilios;Mikros, Emmanuel;Flajolet, Marc;Greengard, Paul;Meijer, Laurent;Galons, Herve;,期刊：Journal of Medicinal Chemistry, 页码：5229-5242 , 文章类型： 研究论文，,卷期：2008年51-17] Cyclin-dependent kinases (CDKs) and casein kinases 1 (CK1) are involved in the two key mol. features of Alzheimer's disease, prodn. of amyloid-b peptides (extracellular plaques) and hyper-phosphorylation of Tau (intracel... Novel Glucagon Receptor Antagonists with Improved Selectivity over the Glucose-Dependent Insulinotropic Polypeptide Receptor. [作者：Kodra, Janos T.;Steen Jorgensen, Anker;Andersen, Birgitte;Behrens, Carsten;Lehn Brand, Christian;Thoeger Christensen, Inger;Guldbrandt, Mette;Bekker Jeppesen, Claus;Knudsen, Lotte B.;Madsen, Peter;Nishimura, Erica;Sams, Christian;Sidelmann, Ulla G.;Peders,期刊：Journal of Medicinal Chemistry, 页码：5387-5396 , 文章类型： 研究论文，,卷期：2008年51-17] Optimization of a new series of small mol. human glucagon receptor (hGluR) antagonists is described. In the process of optimizing glucagon receptor antagonists, we counter-screened against the closely related human gast... 2-(4-(tetrahydro-2H-pyran-2-yloxy)-undecyl)-propane-1,3-diamminedichl oroplatinum(II): A Novel Platinum Compound that Overcomes Cisplatin Resistance and Induces Apoptosis by Mechanisms Different from that of Cisplatin. [作者：Dietrich, Andrea;Mueller, Thomas;Paschke, Reinhard;Kalinowski, Bernd;Behlendorf, Timo;Reipsch, Franziska;Fruehauf, Angelika;Schmoll, Hans-Joachim;Kloft, Charlotte;Voigt, Wieland;,期刊：Journal of Medicinal Chemistry, 页码：5413-5422 , 文章类型： 研究论文，,卷期：2008年51-17] complexes (1-12) consisting of CDDP linked to THP via aliph. CH2-spacers were tested in two TGCT cell lines. The most promising compd., 2-(4-(tetrahydro-2H-pyran-2-yloxy)-undecyl)-propane-1,3-diamminedichl oroplatinum(I... Discovery of the First Potent and Orally Efficacious Agonist of the Orphan G-Protein Coupled Receptor 119. [作者：Semple, Graeme;Fioravanti, Beatriz;Pereira, Guillherme;Calderon, Imelda;Uy, Jane;Choi, Karoline;Xiong, Yifeng;Ren, Albert;Morgan, Michael;Dave, Vibha;Thomsen, William;Unett, David J.;Xing, Charles;Bossie, Stuart;Carroll, Chris;Chu, Zhi-Liang;Grottick, And,期刊：Journal of Medicinal Chemistry, 页码：5172-5175 , 文章类型： 研究论文，,卷期：2008年51-17] GPR119 is a rhodopsin-like GPCR expressed in pancreatic b-cells and incretin releasing cells in the GI tract. As with incretins, GPR119 increases cAMP levels in these cell types, thus making it a highly attractive poten... Inhibition of Siderophore Biosynthesis in Mycobacterium tuberculosis with Nucleoside Bisubstrate Analogues: Structure-Activity Relationships of the Nucleobase Domain of 5'-O-[N-(Salicyl)sulfamoyl]adenosine. [作者：Neres, Joao;Labello, Nicholas P.;Somu, Ravindranadh V.;Boshoff, Helena I.;Wilson, Daniel J.;Vannada, Jagadeshwar;Chen, Liqiang;Barry, Clifton E., III;Bennett, Eric M.;Aldrich, Courtney C.;,期刊：Journal of Medicinal Chemistry, 页码：5349-5370 , 文章类型： 研究论文，,卷期：2008年51-17] 5'-O-[N-(salicyl)sulfamoyl]adenosine (Sal-AMS) is a prototype for a new class of antitubercular agents that inhibit the aryl acid adenylating enzyme (AAAE) known as MbtA involved in biosynthesis of the mycobactins. Here... Novel Dual-Targeting Benzimidazole Urea Inhibitors of DNA Gyrase and Topoisomerase IV Possessing Potent Antibacterial Activity: Intelligent Design and Evolution through the Judicious Use of Structure-Guided Design and Structure-Activity Relationships. [作者：Charifson, Paul S.;Grillot, Anne-Laure;Grossman, Trudy H.;Parsons, Jonathan D.;Badia, Michael;Bellon, Steve;Deininger, David D.;Drumm, Joseph E.;Gross, Christian H.;LeTiran, Arnaud;Liao, Yusheng;Mani, Nagraj;Nicolau, David P.;Perola, Emanuele;Ronkin, Stev,期刊：Journal of Medicinal Chemistry, 页码：5243-5263 , 文章类型： 研究论文，,卷期：2008年51-17] The discovery of new antibacterial agents with novel mechanisms of action is necessary to overcome the problem of bacterial resistance that affects all currently used classes of antibiotics. Bacterial DNA gyrase and top... Modulating G-Protein Coupled Receptor/G-Protein Signal Transduction by Small Molecules Suggested by Virtual Screening. [作者：Taylor, Christina M.;Barda, Yaniv;Kisselev, Oleg G.;Marshall, Garland R.;,期刊：Journal of Medicinal Chemistry, 页码：5297-5303 , 文章类型： 研究论文，,卷期：2008年51-17] Modulation of interactions between activated GPCRs (G-protein coupled receptors) and the intracellular (IC) signal transducers, heterotrimeric G-proteins, is an attractive, yet essentially unexplored, paradigm for treatm... Formal Concept Analysis for the Identification of Molecular Fragment Combinations Specific for Active and Highly Potent Compounds. [作者：Lounkine, Eugen;Auer, Jens;Bajorath, Juergen;,期刊：Journal of Medicinal Chemistry, 页码：5342-5348 , 文章类型： 研究论文，,卷期：2008年51-17] We introduce fragment formal concept anal. (FragFCA) to study complex relationships between fragments in active compds. taking potency information into account. Fragment combinations that are unique to active or highly ... Bioisosteric Replacement of the Pyrazole 5-Aryl Moiety of N-(Piperidin-1-yl)-5-(4-chlorophenyl)-1-(2,4-dichlorophenyl)-4-methyl-1H -pyrazole-3-carboxamide (SR141716A). A Novel Series of Alkynylthiophenes as Potent and Selective Cannabinoid-1 Receptor Anta [作者：Tseng, Shi-Liang;Hung, Ming-Shiu;Chang, Chun-Ping;Song, Jen-Shin;Tai, Chia-Liang;Chiu, Hua-Hao;Hsieh, Wan-Ping;Lin, Yinchiu;Chung, Wan-Ling;Kuo, Chun-Wei;Wu, Chien-Huang;Chu, Cheng-Ming;Tung, Yen-Shih;Chao, Yu-Sheng;Shia, Kak-Shan;,期刊：Journal of Medicinal Chemistry, 页码：5397-5412 , 文章类型： 研究论文，,卷期：2008年51-17] Replacing the conventional pyrazole 5-aryl substituent of 1 (SR141716A) with the 2-thienyl moiety appended with an appropriate alkynyl unit, a novel class of 5-(5-alkynyl-2-thienyl)pyrazole derivs., behaving as highly po... Conformationally Constrained Analogues of Diacylglycerol. 30. An Investigation of Diacylglycerol-lactones Containing Heteroaryl Groups Reveals Compounds with High Selectivity for Ras Guanyl Nucleotide-Releasing Proteins. [作者：El Kazzouli, Said;Lewin, Nancy E.;Blumberg, Peter M.;Marquez, Victor E.;,期刊：Journal of Medicinal Chemistry, 页码：5371-5386 , 文章类型： 研究论文，,卷期：2008年51-17] developed in our lab. as a scaffold with high binding affinity for C1 domains, we describe herein a series of novel DAG-lactones contg. heterocyclic moieties (pyridines, quinolines, and indoles) as a-arylidene fragments.... Novel and Potent Inhibitors of 5-Lipoxygenase Product Synthesis Based on the Structure of Pirinixic Acid. [作者：Werz, Oliver;Greiner, Christine;Koeberle, Andreas;Hoernig, Christina;George, Sven;Popescu, Laura;Syha, Ivonne;Schubert-Zsilavecz, Manfred;Steinhilber, Dieter;,期刊：Journal of Medicinal Chemistry, 页码：5449-5453 , 文章类型： 研究论文，,卷期：2008年51-17] A novel class of potent 5-lipoxygenase (5-LO) product synthesis inhibitors based on the structure of pirinixic acid (4-chloro-6-(2,3-xylidino)-2-pyrimidinylthioacetic acid, compd. 1) is presented. Systematic profiling o... Structure-Activity Relationship Study on Anti-HIV 6-Desfluoroquinolones. [作者：Tabarrini, Oriana;Massari, Serena;Daelemans, Dirk;Stevens, Miguel;Manfroni, Giuseppe;Sabatini, Stefano;Balzarini, Jan;Cecchetti, Violetta;Pannecouque, Christophe;Fravolini, Arnaldo;,期刊：Journal of Medicinal Chemistry, 页码：5454-5458 , 文章类型： 研究论文，,卷期：2008年51-17] On the basis of our recent findings that 6-aminoquinolones inhibit the HIV Tat-mediated transactivation, we have designed a broad series of derivs. identifying novel potent agents such as the 6-desfluoroquinolones 24 (HM... 2-Thiazolylimino/Heteroarylimino-5-arylidene-4-thiazolidinones as New Agents with SHP-2 Inhibitory Action. [作者：Geronikaki, A.;Eleftheriou, P.;Vicini, P.;Alam, I.;Dixit, A.;Saxena, A. K.;,期刊：Journal of Medicinal Chemistry, 页码：5221-5228 , 文章类型： 研究论文，,卷期：2008年51-17] PTPN11 gene, mediates cell signaling by growth factors and cytokines via the RAS/MAP kinase pathway. Somatic mutations in PTPN11 gene account for approx. 18% of juvenile myelomonocytic leukemia (JMML) patients. Moreove... Cytotoxicity, Cellular Uptake, and DNA Interactions of New Monodentate Ruthenium(II) Complexes Containing Terphenyl Arenes. [作者：Bugarcic, Tijana;Novakova, Olga;Halamikova, Anna;Zerzankova, Lenka;Vrana, Oldrich;Kasparkova, Jana;Habtemariam, Abraha;Parsons, Simon;Sadler, Peter J.;Brabec, Viktor;,期刊：Journal of Medicinal Chemistry, 页码：5310-5319 , 文章类型： 研究论文，,卷期：2008年51-17] We have compared the cancer cell cytotoxicity, cell uptake, and DNA binding properties of the isomeric terphenyl complexes [(h6-arene)Ru(en)Cl]+, where the arene is ortho- (2), meta- (3), or para-terphenyl (1) (o-, m-, o...