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.
Eur J Med Chem. 2013 Aug;66:423-37. doi: 10.1016/j.ejmech.2013.06.011. Epub 2013 Jun 18.
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.
一系列新型二苯并[b,d]呋喃-咪唑杂合化合物已经被制备出来，并在体外对一系列人类肿瘤细胞系进行了评估。结果表明，苯并咪唑环的存在以及咪唑基-3-位被萘甲酰基或 4-甲氧基苯甲酰基取代，对于调节细胞毒性活性至关重要。特别是，杂合化合物 60 被发现对所有研究的人类肿瘤细胞系均具有最强的活性，而化合物 49 对乳腺癌（MCF-7）和髓性肝癌（SMMC-7721）具有更高的选择性。化合物 60 可以诱导 SMMC-7721 细胞的 G1 期细胞周期停滞和凋亡。
