期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 78, 期 -, 页码 178-189出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.03.032
关键词
Combretastatin A-4; IsoCA-4; Isoerianin; AzaisoCA-4; Cytotoxicity; Antimitotic; Tubulin
资金
- CNRS (Centre National de la Recherche Scientifique)
- ARC (association pour la recherche sur le cancer)
- ANR (Agence Nationale de la Recherche) [ANR-10-LABX-33]
- ANR [ANR-09-BLAN-0071]
A series of N-methyl-diarylamines 2 was designed and synthesized as a novel class of CA-4 and isoCA-4 analogues. Compounds 2b and 2m showed excellent antiproliferative activity with mean GI(50) values at a nanomolar level in a diverse set of human cancer cells. These compounds also inhibited tubulin assembly at a micromolar range, arrested the cellular cycle in the G2/M phase and induced apoptosis at very low concentrations. Preliminary in vitro results revealed that 2b and 2m displayed substantial efficacy as potent antivascular agents. Docking studies indicates that these lead compounds showed a binding mode similar to those observed with isoCA-4 at the colchicine binding site of tubulin. (C) 2014 Elsevier Masson SAS. All rights reserved.
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