期刊
ARCHIV DER PHARMAZIE
卷 347, 期 11, 页码 853-860出版社
WILEY-V C H VERLAG GMBH
DOI: 10.1002/ardp.201400215
关键词
Apoptosis; Anti-cancer agents; Chalcone; Cytotoxicity; Flavanone
资金
- Tehran University of Medical Sciences
- Iran National Science Foundation (INSF)
A novel series of chalcones and flavanones discriminated by the presence of a 3,4-dimethoxyphenyl moiety in their structures were synthesized as anti-cancer agents. The cytotoxicity evaluation of the analogs against the MCF-7, MDA-MB-231 (human breast cancer), and SK-N-MC (human neuroblastoma) cell lines demonstrated that the introduction of a halogen on the 3,4-dimethoxyphenyl part of both series and the attachment of a pyrrolidinylethoxy group on the C-7 position of the flavanone derivatives increased their activity. Indeed, 3-halogenated chalcones (1c and 1d) were more potent than the standard drug etoposide against all tested cell lines. Fluorescence microscopy and flow cytometry analyses confirmed that the anti-cancer effect of the most potent compounds 1c and 1d occurs via apoptosis induction.
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