- Knowledge-based analysis of multi-potent G-protein coupled receptors ligands
[作者:Faure, P; Dubus, E; Ijjaali, I; Morliere, C; Barberan, O; Petitet, F,期刊:European Journal of Medicinal Chemistry, 页码:5708-5717 , 文章类型: Article,,卷期:2010年45-12]
- A large number of chemical structures that interact with G-protein coupled receptors (GPCRs) have been disclosed in patents or published papers. Most of these compounds are selective for a given protein target; however, ...
- Novel 6-[(hetero)arylamino]thieno[3,2-b]pyridines: Synthesis and antitumoral activities
[作者:Queiroz, MJRP; Calhelha, RC; Vale-Silva, LA; Pinto, E; Nascimento, MSJ,期刊:European Journal of Medicinal Chemistry, 页码:5732-5738 , 文章类型: Article,,卷期:2010年45-12]
- Several novel 6-[(hetero)arylamino]thieno[3,2-b]pyridines were prepared by palladium-catalyzed C-N Buchwald-Hartwig coupling of the methyl 3-amino-6-bromothieno[3,2-b]pyridine-2-carboxylate with aryl and heteroarylamines...
- Synthesis and in vitro biological evaluation of new polyamine conjugates as potential anticancer drugs
[作者:Szumilak, M; Szulawska-Mroczek, A; Koprowska, K; Stasiak, M; Lewgowd, W; Stanczak, A; Czyz, M,期刊:European Journal of Medicinal Chemistry, 页码:5744-5751 , 文章类型: Article,,卷期:2010年45-12]
- The synthesis of new polyamine derivatives containing dimeric quinoline (3a-c), cinnoline (4a-c) and phthalimide (7a-c and 8a-c) moieties is described. Three different polyamines: (1,4-bis(3-aminopropyl) piperazine (a), ...
- Lead identification of conformationally restricted beta-lactam type combretastatin analogues: Synthesis, antiproliferative activity and tubulin targeting effects
[作者:Carr, M; Greene, LM; Knox, AJS; Lloyd, DG; Zisterer, DM; Meegan, MJ,期刊:European Journal of Medicinal Chemistry, 页码:5752-5766 , 文章类型: Article,,卷期:2010年45-12]
- The synthesis and study of the structure activity relationships of a series of rigid analogues of combretastatin A-4 are described which contain the 1,4-diaryl-2-azetidinone (beta-lactam) ring system in place of the usua...
- Massive screening yields novel and selective Trypanosoma cruzi triosephosphate isomerase dimer-interface-irreversible inhibitors with anti-trypanosomal activity
[作者:Alvarez, G; Aguirre-Lopez, B; Varela, J; Cabrera, M; Merlino, A; Lopez, GV; Lavaggi, ML; Porcal, W; Di Maio, R; Gonzalez, M; Cerecetto, H; Cabrera, N; Perez-Montfort, R; de Gomez-Puyou, MT; Gomez-Puyou, A,期刊:European Journal of Medicinal Chemistry, 页码:5767-5772 , 文章类型: Article,,卷期:2010年45-12]
- Triosephosphate isomerase from Trypanosoma cruzi (TcTIM), an enzyme in the glycolytic pathway that exhibits high catalytic rates of glyceraldehyde-3-phosphate- and dihydroxyacetone-phosphate-isomerization only in its dim...
- Synthesis and anti-inflammatory evaluation of novel mono-carbonyl analogues of curcumin in LPS-stimulated RAW 264.7 macrophages
[作者:Zhao, CG; Cai, YP; He, XZ; Li, JL; Zhang, L; Wu, JZ; Zhao, YJ; Yang, SL; Li, XK; Li, WL; Liang, GA,期刊:European Journal of Medicinal Chemistry, 页码:5773-5780 , 文章类型: Article,,卷期:2010年45-12]
- Curcumin is a multifunctional natural product with regulatory effects on inflammation. However, a major limitation for the application of curcumin is its poor bioavailability. We previously demonstrated that the mono-car...
- Synthesis and biological evaluation of 2-(3 ',4 ',5 '-trimethoxybenzoyl)-3-aryl/arylaminobenzo[b]thiophene derivatives as a novel class of antiproliferative agents
[作者:Romagnoli, R; Baraldi, PG; Cara, CL; Hamel, E; Basso, G; Bortolozzi, R; Viola, G,期刊:European Journal of Medicinal Chemistry, 页码:5781-5791 , 文章类型: Article,,卷期:2010年45-12]
- The biological importance of microtubules in mitosis, as well as in interphase, makes them an interesting target for the development of anticancer agents. Small molecules such as benzo[b]thiophenes are attractive as inhi...
- Synthesis, crystal structure and biological evaluation of novel 2-(5-(hydroxymethyl)-3-phenyl-1H-pyrazol-1-yl)-1-phenylethanol derivatives
[作者:Zheng, LW; Zhu, JA; Zhao, BX; Huang, YH; Ding, J; Miao, JY,期刊:European Journal of Medicinal Chemistry, 页码:5792-5799 , 文章类型: Article,,卷期:2010年45-12]
- A series of novel 2-(5-(hydroxymethyl)-3-phenyl-1H-pyrazol-1-yl)-1-phenylethanol derivatives (4) was synthesized from ethyl 1-(2-oxo-2-phenylethyl)-3-phenyl-1H-pyrazole-5-carboxylate derivatives (3) and characterized by ...
- Synthesis and alpha(1)-adrenoceptor antagonist activity of tamsulosin analogues
[作者:Sagratini, G; Angeli, P; Buccioni, M; Gulini, U; Marucci, G; Melchiorre, C; Poggesi, E; Giardina, D,期刊:European Journal of Medicinal Chemistry, 页码:5800-5807 , 文章类型: Article,,卷期:2010年45-12]
- Tamsulosin (-)-1 is the most utilized alpha(1)-adrenoceptor antagonist in the benign prostatic hyperplasia therapy owing to its uroselective antagonism and capability in relieving both obstructive and irritative lower ur...
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