- Design, synthesis and evaluation of caffeic acid phenethyl ester-based inhibitors targeting a selectivity pocket in the active site of human aldo-keto reductase 1B10
[作者:Soda, M; Hu, DW; Endo, S; Takemura, M; Li, J; Wada, R; Ifuku, S; Zhao, HT; El-Kabbani, O; Ohta, S; Yamamura, K; Toyooka, N; Hara, A; Matsunaga, T,期刊:European Journal of Medicinal Chemistry, 页码:321-329 , 文章类型: Article,,卷期:2012年48-1]
- Inhibitors of a human aldo keto reductase, AKR1B10, are regarded as promising therapeutics for the treatment of cancer, but those with both high potency and selectivity compared to the structurally similar aldose reducta...
- Synthesis and anticonvulsant activity of 1-(8-(benzyloxy)quinolin-2-y1)-6substituted-4,6-diazaspiro[2,4]heptane-5,7-diones
[作者:He, XR; Zhong, M; Zhang, T; Yang, J; Wu, ZY; Xiao, YL; Guo, H; Qiu, GF; Hu, XM,期刊:European Journal of Medicinal Chemistry, 页码:338-346 , 文章类型: Article,,卷期:2012年48-1]
- In the present study on the development of new anticonvulsants, 16 new1-(8-(benzyloxy)quinolin-2-yl-6-substituted-4,6-diazaspiro[2,4]heptane-5,7-diones were synthesized and tested for anticonvulsant activity using the ma...
- Synthesis and anticonvulsant activity of novel 2,6-diketopiperazine derivatives. Part 2: Perhydropyrido[1,2-a]pyrazines
[作者:Dawidowski, M; Herold, F; Chodkowski, A; Kleps, J,期刊:European Journal of Medicinal Chemistry, 页码:347-353 , 文章类型: Article,,卷期:2012年48-1]
- A new series of chiral pyrido[1,2-a]pyrazine derivatives was synthesised and evaluated in in vivo animal models of epilepsy. A significant influence of the stereochemistry of the pyrido[1,2-a]pyrazine framework on the ph...
- Proton-pumping-ATPase-targeted antifungal activity of cinnamaldehyde based sulfonyl tetrazoles
[作者:Shreaz, S; Wani, MY; Ahmad, SR; Ahmad, SI; Bhatia, R; Athar, F; Nikhat, M; Khan, LA,期刊:European Journal of Medicinal Chemistry, 页码:363-370 , 文章类型: Article,,卷期:2012年48-1]
- Azoles are generally fungistatic, and resistance to fluconazole is emerging in several fungal pathogens. We designed a series of cinnamaldehyde based sulfonyl tetrazole derivatives. To further explore the antifungal acti...
- A concise synthesis of viscolin, and its anti-inflammatory effects through the suppression of iNOS, COX-2, ERK phosphorylation and proinflammatory cytokines expressions
[作者:Huang, GJ; Reddy, MVB; Kuo, PC; Huang, CH; Shih, HC; Lee, EJ; Yang, ML; Leu, YL; Wu, TS,期刊:European Journal of Medicinal Chemistry, 页码:371-378 , 文章类型: Article,,卷期:2012年48-1]
- In the present report, a concise synthesis of viscolin (1) has been achieved. The anti-inflammatory effect of viscolin was investigated in vitro and in vivo. Viscolin blocked the expression of iNOS and COX-2, and it also...
- Synthesis and cytotoxicity of O,O '-dialkyl {[2-(substituted phenoxy) acetamido](substituted phenyl)methyl}phosphonates
[作者:Ning, LH; Wang, W; Liang, YJ; Peng, H; Fu, LW; He, HW,期刊:European Journal of Medicinal Chemistry, 页码:379-384 , 文章类型: Article,,卷期:2012年48-1]
- A series of O,O'-dialkyl {[2-(substituted phenoxy)acetamido](substituted phenyl)methyl}phosphonates was synthesized and their cytotoxic activities were tested against various human tumor cell lines. Some compounds (5q, 5...
- Synthesis, antiproliferative activity and estrogen receptor alpha affinity of novel estradiol-linked platinum(II) complex analogs to carboplatin and oxaliplatin. Potential vector complexes to target estrogen-dependent tissues
[作者:Saha, P; Descoteaux, C; Brasseur, K; Fortin, S; Leblanc, V; Parent, S; Asselin, E; Berube, G,期刊:European Journal of Medicinal Chemistry, 页码:385-390 , 文章类型: Article,,卷期:2012年48-1]
- In the course of efforts to develop 17 beta-estradiol-linked to anticancer agents targeting estrogen-dependent tissue, we identified three estradiol-linked platinum(II) complex analogs to cisplatin (E-CDDP) derivatives n...
- Design, synthesis and biological evaluation of pyrazole derivatives as potential multi-kinase inhibitors in hepatocellular carcinoma
[作者:Strocchi, E; Fornari, F; Minguzzi, M; Gramantieri, L; Milazzo, M; Rebuttini, V; Breviglieri, S; Camaggi, CM; Locatelli, E; Bolondi, L; Comes-Franchini, M,期刊:European Journal of Medicinal Chemistry, 页码:391-401 , 文章类型: Article,,卷期:2012年48-1]
- We described the optimization, by molecular modelling, of small pyrazole derivatives, as kinase inhibitors, obtained through a 1,3-dipolar cycloaddition between nitrile imines and functionalized acetylenes. The two compo...
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