- 4,4-Dimethyl-1,2,3,4-tetrahydroquinoline-based PPAR alpha/gamma agonists. Part. II: Synthesis and pharmacological evaluation of oxime and acidic head group structural variations
[作者:Parmenon, C; Guillard, J; Caignard, DH; Hennuyer, N; Staels, B; Audinot-Bouchez, V; Boutin, JA; Dacquet, C; Ktorza, A; Viaud-Massuard, MC,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2683-2687 , 文章类型: Article,,卷期:2009年19-10]
- Type-2 diabetes (T2D) is a complex metabolic disease characterized by insulin resistance in the liver and peripheral tissues accompanied by a deficiency in pancreatic beta-cells. Since their discovery, three subtypes of ...
- Microwave assisted synthesis of new indophenazine 1,3,5-trisubstruted pyrazoline derivatives of benzofuran and their antimicrobial activity
[作者:Manna, K; Agrawal, YK,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2688-2692 , 文章类型: Article,,卷期:2009年19-10]
- 2-[1-(5,8-Dihydro quinoxalino[2,3-b]indoloacetyl)-3-(1-benzofuran-2-yl)-4,5-dihydro-1H-pyrazol-5-yl] phenyl derivatives were synthesized from 2-(5,8-dihydro quinoxalino[2,3-b]indol-5-yl) acetohydrazide and (2E)-1-(1-benz...
- Discovery of thioether-bridged cyclic pentapeptides binding to Grb2-SH2 domain with high affinity
[作者:Jiang, S; Liao, CZ; Bindu, L; Yin, BL; Worthy, KW; Fisher, RJ; Burke, TR; Nicklaus, MC; Roller, PP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2693-2698 , 文章类型: Article,,卷期:2009年19-10]
- Blocking the interaction between phosphotyrosine (pTyr)-containing activated receptors and the Src homology 2 (SH2) domain of the growth factor receptor-bound protein 2 (Grb 2) is considered to be an effective and non-cy...
- Synthetic studies in butenonyl C-glycosides: Preparation of polyfunctional alkanonyl glycosides and their enzyme inhibitory activity
[作者:Bisht, SS; Fatima, S; Tamrakar, AK; Rahuja, N; Jaiswal, N; Srivastava, AK; Tripathi, RP,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2699-2703 , 文章类型: Article,,卷期:2009年19-10]
- A simple synthesis of phenyl butenoyl C-glycosides has been achieved by Aldol condensation of peracetylated glycosyl acetones with aromatic aldehydes followed by deacetylation with methanolic NaOMe. The selected butenoyl...
- Cytotoxicity and structure-activity relationships of four alpha-N-heterocyclic thiosemicarbazone derivatives crystal structure of 2-acetylpyrazine thiosemicarbazone
[作者:Li, MX; Chen, CL; Ling, CS; Zhou, J; Ji, BS; Wu, YJ; Niu, JY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2704-2706 , 文章类型: Article,,卷期:2009年19-10]
- A series of thiosemicarbazone ligands, HL1 (2-acetylpyrazine thiosemicarbazone), HL2 (2-acetylpyrazine N(4)-methylthiosemicarbazone), HL3 (2-benzoylpyridine thiosemicarbazone) and HL4 (2-benzoylpyridine N(4)-methylthiose...
- Discovery of substituted N '-(2-oxoindolin-3-ylidene)benzohydrazides as new apoptosis inducers using a cell- and caspase-based HTS assay
[作者:Sirisoma, N; Pervin, A; Drewe, J; Tseng, B; Cai, SX,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2710-2713 , 文章类型: Article,,卷期:2009年19-10]
- We report the discovery of a series of substituted N'-(2-oxoindolin-3-ylidene)benzohydrazides as inducers of apoptosis using our proprietary cell- and caspase-based ASAP HTS assay. Through SAR studies, N'-(4-bromo-5-meth...
- Examination of halogen substituent effects on HIV-1 integrase inhibitors derived from 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-ones and 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones
[作者:Zhao, XZ; Maddali, K; Vu, BC; Marchand, C; Hughes, SH; Pommier, Y; Burke, TR,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2714-2717 , 文章类型: Article,,卷期:2009年19-10]
- Using 2,3-dihydro-6,7-dihydroxy-1H-isoindol-1-one and 4,5-dihydroxy-1H-isoindole-1,3(2H)-dione based HIV-1 integrase inhibitors as display platforms, we undertook a thorough examination of the effects of modifying the ha...
- Discovery of novel 3,6-disubstituted 2-pyridinecarboxamide derivatives as GK activators
[作者:Mitsuya, M; Kamata, K; Bamba, M; Watanabe, H; Sasaki, Y; Sasaki, K; Ohyama, S; Hosaka, H; Nagata, Y; Eiki, J; Nishimura, T,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2718-2721 , 文章类型: Article,,卷期:2009年19-10]
- A novel class of 3,6-disubstituted 2-pyridinecarboxamide derivatives was designed based on X-ray analysis of the 2-aminobenzamide lead class. Subsequent chemical modi. cation led to the discovery of potent GK activators ...
- New developments for the design, synthesis and biological evaluation of potent SARS-CoV 3CL(pro) inhibitors
[作者:Regnier, T; Sarma, D; Hidaka, K; Bacha, U; Freire, E; Hayashi, Y; Kiso, Y,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2722-2727 , 文章类型: Article,,卷期:2009年19-10]
- A series of trifluoromethyl, benzothiazolyl or thiazolyl ketone-containing peptidic compounds as SARS-CoV 3CL protease inhibitors were developed and their potency was evaluated by in vitro protease inhibitory assays. Thr...
- Two novel monoterpene-chalcone conjugates isolated from the seeds of Alpinia katsumadai
[作者:Hua, SZ; Luo, JG; Wang, XB; Wang, JS; Kong, LY,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2728-2730 , 文章类型: Article,,卷期:2009年19-10]
- Three monoterpene-chalcone conjugates, including two novel compounds isorubraine (2) and sumadain C (3), and a known compound rubraine (1) were isolated from the seeds of Alpinia katsumadai. Their structures and relative...
- Quaternary ammonium N,N-dichloroamines as topical, antimicrobial agents
[作者:Francavilla, C; Low, E; Nair, S; Kim, B; Shiau, TP; Debabov, D; Celeri, C; Alvarez, N; Houchin, A; Xu, P; Najafi, R; Jain, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2731-2734 , 文章类型: Article,,卷期:2009年19-10]
- A series of backbone modified and sulfonic acid replacement analogs of our topical, clinical candidate (iii) were synthesized. Their antimicrobial activities and aqueous stabilities at pH 4 and pH 7 were determined, and ...
- Identification of pyrazolo[1,5-a]pyrimidine-3-carboxylates as B-Raf kinase inhibitors
[作者:Gopalsamy, A; Ciszewski, G; Hu, YB; Lee, F; Feldberg, L; Frommer, E; Kim, S; Collins, K; Wojciechowicz, D; Mallon, R,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2735-2738 , 文章类型: Article,,卷期:2009年19-10]
- B-Raf kinase plays a critical role in the Raf-MEK-ERK signaling pathway and inhibitors of B-Raf could be used in the treatment of melanomas, colorectal cancer, and other Ras related human cancers. We have identified nove...
- Synthesis and anticancer activities of novel 3,5-disubstituted-1,2,4-oxadiazoles
[作者:Kumar, D; Patel, G; Johnson, EO; Shah, K,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2739-2741 , 文章类型: Article,,卷期:2009年19-10]
- A series of 3,5-disubstituted-1,2,4-oxadiazoles were synthesized and evaluated for their in vitro anti-proliferative activities against various cancer cell lines. Formation of 1,2,4-oxadiazole ring was accomplished by th...
- Constrained (L-)-S-adenosyl-L-homocysteine (SAH) analogues as DNA methyltransferase inhibitors
[作者:Isakovic, L; Saavedra, OM; Llewellyn, DB; Claridge, S; Zhan, LJ; Bernstein, N; Vaisburg, A; Elowe, N; Petschner, AJ; Rahil, J; Beaulieu, N; Gauthier, F; MacLeod, AR; Delorme, D; Besterman, JM; Wahhab, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2742-2746 , 文章类型: Article,,卷期:2009年19-10]
- Potent SAH analogues with constrained homocysteine units have been designed and synthesized as inhibitors of human DNMT enzymes. The five membered (2S,4S)-4-mercaptopyrrolidine-2-carboxylic acid, in 1a, was a good replac...
- SAR around (L)-S-adenosyl-L-homocysteine, an inhibitor of human DNA methyltransferase (DNMT) enzymes
[作者:Saavedra, OM; Isakovic, L; Llewellyn, DB; Zhan, LJ; Bernstein, N; Claridge, S; Raeppel, F; Vaisburg, A; Elowe, N; Petschner, AJ; Rahil, J; Beaulieu, N; MacLeod, AR; Delorme, D; Besterman, JM; Wahhab, A,期刊:Bioorganic & Medicinal Chemistry Letters, 页码:2747-2751 , 文章类型: Article,,卷期:2009年19-10]
- The inhibitory activity of base-modified SAH analogues and the specificity of inhibiting human DNMT1 and DNMT3b2 enzymes was explored. The 6-amino group was essential while the 7-N of the adenine ring of SAH could be rep...
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