期刊
EUROPEAN JOURNAL OF MEDICINAL CHEMISTRY
卷 95, 期 -, 页码 492-499出版社
ELSEVIER FRANCE-EDITIONS SCIENTIFIQUES MEDICALES ELSEVIER
DOI: 10.1016/j.ejmech.2015.03.057
关键词
Anti-cancer; Cytotoxic agents; 3H-quinazolin-4-one; trans-stilbene
资金
- Research Council of Tehran University of Medical Sciences
- Iran National Science Foundation (INSF)
A novel series of 2-arylquinazolinones 7a-o bearing trans-stilbene moiety were designed, synthesized, and evaluated against human breast cancer cell lines including human breast adenocarcinoma (MCF-7 and MDA-MB-231) and human ductal breast epithelial tumor (T-47D). Among the tested compounds, the sec-butyl derivative 7h showed the best profile of activity (IC50 < 5 mu M) against all cell lines, being 2-fold more potent than standard drug, etoposide. Our investigation revealed that the cytotoxic activity was significantly affected by N3-alkyl substituents. Furthermore, the morphological analysis by acridine orange/ethidium bromide double staining test and flow cytometry analysis indicated that the prototype compound 7h can induce apoptosis in MCF-7 and MDA-MB-231 cells. (C) 2015 Elsevier Masson SAS. All rights reserved.
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