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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44条记录   N9-Substituted 2,4-Diaminoquinazolines: Synthesis and Biological Evaluation of Lipophilic Inhibitors of Pneumocystis carinii and Toxoplasma gondii Dihydrofolate Reductase. [作者：Gangjee, Aleem;Adair, Ona O.;Pagley, Michelle;Queener, Sherry F.;,期刊：Journal of Medicinal Chemistry, 页码：6195-6200 , 文章类型： 研究论文，,卷期：2008年51-19] N9-substituted 2,4-diaminoquinazolines were synthesized and evaluated as inhibitors of Pneumocystis carinii (pc) and Toxoplasma gondii (tg) dihydrofolate reductase (DHFR). Redn. of com. available 2,4-diamino-6-nitroquin... Potent s-cis-Locked Bithiazole Correctors of DF508 Cystic Fibrosis Transmembrane Conductance Regulator Cellular Processing for Cystic Fibrosis Therapy. [作者：Yu, Gui Jun;Yoo, Choong L.;Yang, Baoxue;Lodewyk, Michael W.;Meng, Liping;El-Idreesy, Tamer T.;Fettinger, James C.;Tantillo, Dean J.;Verkman, A. S.;Kurth, Mark J.;,期刊：Journal of Medicinal Chemistry, 页码：6044-6054 , 文章类型： 研究论文，,卷期：2008年51-19] N-(5-(2-(5-Chloro-2-methoxyphenylamino)thiazol-4-yl)-4-methylthiazol-2 -yl)pivalamide I (R1 = Me; R2 = H; R3 = 5-Cl-2-MeOC6H3) was found previously to correct defective cellular processing of the cystic fibrosis protein ... New Chimeric Antimalarials with 4-Aminoquinoline Moiety Linked to a Tetraoxane Skeleton. [作者：Opsenica, Igor;Opsenica, Dejan;Lanteri, Charlotte Anne;Anova, Lalaine;Milhous, Wilbur K.;Smith, Kirsten S.;Solaja, Bogdan A.;,期刊：Journal of Medicinal Chemistry, 页码：6216-6219 , 文章类型： 研究论文，,卷期：2008年51-19] The synthesis of the chimeric mols. consisting of two pharmacophores, tetraoxane and 7-chloro-4-aminoquinoline, is reported. The tetraoxanes I, II, and III show relatively potent in vitro antimalarial activities, with I... Dipeptide Boronic Acid Inhibitors of Dipeptidyl Peptidase IV: Determinants of Potency and in Vivo Efficacy and Safety. [作者：Connolly, Beth A.;Sanford, David G.;Chiluwal, Amrita K.;Healey, Sarah E.;Peters, Diane E.;Dimare, Matthew T.;Wu, Wengen;Liu, Yuxin;Maw, Hlaing;Zhou, Yuhong;Li, Youhua;Jin, Zhiping;Sudmeier, James L.;Lai, Jack H.;Bachovchin, William W.;,期刊：Journal of Medicinal Chemistry, 页码：6005-6013 , 文章类型： 研究论文，,卷期：2008年51-19] Dipeptidyl peptidase IV (DPP-IV; E.C. 3.4.14.5), a serine protease that degrades the incretin hormones GLP-1 and GIP, is now a validated target for the treatment of type 2 diabetes. Dipeptide boronic acids, among the fi... Novel Amiodarone-Doxorubicin Cocktail Liposomes Enhance Doxorubicin Retention and Cytotoxicity in DU145 Human Prostate Carcinoma Cells. [作者：Theodossiou, Theodossis A.;Galanou, Maria C.;Paleos, Constantinos M.;,期刊：Journal of Medicinal Chemistry, 页码：6067-6074 , 文章类型： 研究论文，,卷期：2008年51-19] We have developed novel cocktail liposomes bearing doxorubicin in their hydrophilic cores, and amiodarone, a potent multidrug resistance inhibitor, in their lipid bilayers. The efficacy of these liposomes was studied in... Desferrithiocin Analogues and Nephrotoxicity. [作者：Bergeron, Raymond J.;Wiegand, Jan;McManis, James S.;Bharti, Neelam;Singh, Shailendra;,期刊：Journal of Medicinal Chemistry, 页码：5993-6004 , 文章类型： 研究论文，,卷期：2008年51-19] The syntheses of a series of 4'-O-alkylated (S)-4,5-dihydro-2-(2,4-dihydroxyphenyl)-4-methyl-4-thiazolecarboxylic acid and 5'-O-alkylated (S)-4,5-dihydro-2-(2,5-dihydroxyphenyl)-4-methyl-4-thiazolecarboxylic acid ligands... Structure-Activity Relationships for a Novel Series of Dopamine D2-like Receptor Ligands Based on N-Substituted 3-Aryl-8-azabicyclo[3.2.1]octan-3-ol. [作者：Paul, Noel M.;Taylor, Michelle;Kumar, Rakesh;Deschamps, Jeffrey R.;Luedtke, Robert R.;Newman, Amy Hauck;,期刊：Journal of Medicinal Chemistry, 页码：6095-6109 , 文章类型： 研究论文，,卷期：2008年51-19] Discovering dopamine D2-like receptor subtype-selective ligands has been a focus of significant investigation. The D2R-selective antagonist 3-[4-(4-chlorophenyl)-4-hydroxypiperidinyl]methylindole (L741,626; Ki(D2R/D3R) ... Flexible Side Chain Models Improve Enrichment Rates in In Silico Screening. [作者：Kokh, Daria B.;Wenzel, Wolfgang;,期刊：Journal of Medicinal Chemistry, 页码：5919-5931 , 文章类型： 研究论文，,卷期：2008年51-19] affinity calcns. remain challenging and enrichment rates of in silico screening methods unsatisfactory. Inadequate treatment of induced fit effects is one major shortcoming of existing in silico screening methods. Here... Novel Aldosterone Synthase Inhibitors with Extended Carbocyclic Skeleton by a Combined Ligand-Based and Structure-Based Drug Design Approach. [作者：Lucas, Simon;Heim, Ralf;Negri, Matthias;Antes, Iris;Ries, Christina;Schewe, Katarzyna E.;Bisi, Alessandra;Gobbi, Silvia;Hartmann, Rolf W.;,期刊：Journal of Medicinal Chemistry, 页码：6138-6149 , 文章类型： 研究论文，,卷期：2008年51-19] (CYP11B2) inhibitors triggered the design of compds. 11 and 12 by extending a previously established naphthalene mol. scaffold (e.g., present in mols. 1 and 2) via introduction of a Ph or benzyl residue in 3-position. T... Discovery and Evaluation of 4-(2-(4-chloro-1H-pyrazol-1-yl)ethylamino)-3-(6-(1-(3-fluoropropyl)piperi din-4-yl)-4-methyl-1H-benzo[d]imidazol-2-yl)pyridin-2(1H)-one (BMS-695735), an Orally Efficacious Inhibitor of Insulin-like Growth Factor-1 Receptor Kina [作者：Velaparthi, Upender;Wittman, Mark;Liu, Peiying;Carboni, Joan M.;Lee, Francis Y.;Attar, Ricardo;Balimane, Praveen;Clarke, Wendy;Sinz, Michael W.;Hurlburt, Warren;Patel, Karishma;Discenza, Lorell;Kim, Sean;Gottardis, Marco;Greer, Ann;Li, Aixin;Saulnier, Mar,期刊：Journal of Medicinal Chemistry, 页码：5897-5900 , 文章类型： 研究论文，,卷期：2008年51-19] We previously reported that 1 (BMS-536924), a benzimidazole inhibitor of the insulin-like growth factor-1 receptor, had demonstrated in vivo antitumor activity. This lead compd. was found to have potent CYP3A4 inhibitio... An adamantyl-substituted retinoid-derived molecule that inhibits cancer cell growth and angiogenesis by inducing apoptosis and binds to small heterodimer partner nuclear receptor: effects of modifying its carboxylate group on apoptosis, proliferation, and [作者：Dawson, Marcia I.;Xia, Zebin;Liu, Gang;Ye, Mao;Fontana, Joseph A.;Farhana, Lulu;Patel, Bhamik B.;Arumugarajah, Sankari;Bhuiyan, Mohammad;Zhang, Xiao-Kun;Han, Young-Hoon;Stallcup, William B.;Fukushi, Jun-ichi;Mustelin, Tomas;Tautz, Lutz;Su, Ying;Harris, Da,期刊：Journal of Medicinal Chemistry, 页码：6236-6236 , 文章类型： 研究论文，,卷期：2008年51-19] the fourth author, who is affiliated with Cancer Center, Burnham Institute for Medical Research. The correct author listing is given. Hunter-Killer Peptide for Targeted Therapy. [作者：Ellerby, H. Michael;Bredesen, Dale E.;Fujimura, Satoshi;John, Varghese;,期刊：Journal of Medicinal Chemistry, 页码：5887-5892 , 文章类型： 综述，,卷期：2008年51-19] A review. The review discusses potential applications of Hunter-killer peptides as antitumor, antiarthritic, and antiobesity agents.