期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 86, 期 -, 页码 562-569出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2014.09.017
关键词
Anti-cancer agents; Apoptosis; Caspase-3; 2H-chromene; beta-Nitrostyrene
资金
- Research Council of Tehran University of Medical Sciences
- Iran National Science Foundation (INSF)
A series of 2-aryl-3-nitro-2H-chromenes 4a-u were designed as hybrid analogs of flavanone, beta-nitrostyrene and nitrovinylstilbene scaffolds. They were synthesized from the reaction of appropriate beta-nitrostyrenes and salicylaldehydes in good yields. In vitro cytotoxic activities of compounds 4a-u were tested against breast cancer cell lines including MCF-7, T-47D and MDA-MB-231. Most compounds exhibited good cytotoxic activity against selected cell lines, being more potent than standard drug etoposide. Representatively, 8-methoxy-3-nitro-2-(4-chloropheny1)-2H-chromene (4l) with IC50 = 0.2 mu M against MCF-7 cells, was 36-times more potent than etoposide. Apoptosis as a mechanism of cell death for selected compounds 4h and 4l was confirmed morphologically by acridine orange/ ethidium bromide double staining and TUNEL analysis, as well as caspase-3 activation assay. (C) 2014 Elsevier Masson SAS. All rights reserved.
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