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Synthesis and Anticancer Activity of N -Substituted 2-Arylquinazolinones Bearing Trans -Stilbene Scaffold Publisher Pubmed



Mahdavi M1 ; Pedrood K2 ; Safavi M3 ; Saeedi M4, 5 ; Pordeli M6 ; Ardestani SK6 ; Emami S7 ; Adib M2 ; Foroumadi A1 ; Shafiee A1
Authors
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Authors Affiliations
  1. 1. Department of Medicinal Chemistry, Faculty of Pharmacy and Pharmaceutical Sciences Research Center, Tehran University of Medical Sciences, Tehran, 14176, Iran
  2. 2. School of Chemistry, College of Science, University of Tehran, PO Box 14155-6455, Tehran, Iran
  3. 3. Department of Biotechnology, Iranian Research Organization for Science and Technology, Tehran, Iran
  4. 4. Medicinal Plants Research Center, Tehran University of Medical Sciences, Tehran, Iran
  5. 5. Persian Medicine and Pharmacy Research Center, Tehran University of Medical Sciences, Tehran, Iran
  6. 6. Department of Biochemistry, Institute of Biochemistry and Biophysics, University of Tehran, Tehran, Iran
  7. 7. Department of Medicinal Chemistry and Pharmaceutical Sciences Research Center, Faculty of Pharmacy, Mazandaran University of Medical Sciences, Sari, Iran

Source: European Journal of Medicinal Chemistry Published:2015


Abstract

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 μM) 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. © 2015 Elsevier Masson SAS. © 2015 Elsevier Masson SAS.