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  • Title: Synthesis and anticancer activity of N-substituted 2-arylquinazolinones bearing trans-stilbene scaffold.
    Author: Mahdavi M, Pedrood K, Safavi M, Saeedi M, Pordeli M, Ardestani SK, Emami S, Adib M, Foroumadi A, Shafiee A.
    Journal: Eur J Med Chem; 2015 May 05; 95():492-9. PubMed ID: 25847767.
    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.
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