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Eur J Med Chem. 2013 Aug;66:423-37. doi: 10.1016/j.ejmech.2013.06.011. Epub 2013 Jun 18.

Synthesis and antitumor activities of novel dibenzo[b,d]furan-imidazole hybrid compounds.

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Key Laboratory of Medicinal Chemistry for Natural Resource (Yunnan University), Ministry of Education, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China.


A series of novel hybrid compounds between dibenzo[b,d]furan and imidazole has been prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the existence of benzimidazole ring, and the substitution of the imidazolyl-3-position with a naphthylacyl or 4-methoxyphenacyl group, were vital for modulating cytotoxic activity. In particular, hybrid compound 60 was found to be the most potent derivatives against all of human tumor cell lines investigated, while compound 49 was found to be more selective against breast carcinoma (MCF-7) and myeloid liver carcinoma (SMMC-7721). Compound 60 can induce the G1 phase cell cycle arrest and apoptosis in SMMC-7721 cells.


Antitumor activities; Dibenzo[b,d]furan; Hybrid compound; Imidazole; Structure–activity relationships

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