期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 89, 期 -, 页码 115-127出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.10.041
关键词
Indolizine; Microtubule; Melanoma; [3+2] Cycloaddition; Antitubulin; Anticancer agent; 5,6-Fused bicyclic heteroaromatic
资金
- Romanian Ministry of Education, CNCS-UEFISCDI [PN-II-RU-PD-2012-3-0426]
With the aim of investigating new analogues of phenstatin with an indolizin-3-yl unit, in particular as the B-ring, three new series of compounds (6-8, 9-34 and 54) were synthesized and tested for interactions with tubulin polymerization and evaluated for cytotoxicity on an NCI-60 human cancer cell lines panel. The replacement of the 3'-hydroxy-4'-methoxyphenyl B-ring of phenstatin with substituted indolizine unit results in the conservation of both antitubulin and cytotoxic effect. Indolizines 9 and 17 were the most effective in the present study and showed the highest antiproliferative effect on melanoma cell lines MDA-MB-435 (GI(50) = 30 nM) and could serve as new lead compounds for the development of anti-cancer therapeutics. (C) 2014 Elsevier Masson SAS. All rights reserved.
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