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 Apr;62:111-21. doi: 10.1016/j.ejmech.2012.12.040. Epub 2013 Jan 3.
A series of novel hybrid compounds between 2-benzylbenzofuran 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 substitution of the imidazolyl-3-position with a naphthylacyl or 4-methoxyphenacyl group were vital for modulating cytotoxic activity. In particular, hybrid compounds 46 and 47 were found to be the most potent derivatives against 5 strains human tumor cell lines and more active than cisplatin (DDP), and exhibited cytotoxic activities selectively against breast carcinoma (MCF-7) and myeloid liver carcinoma (SMMC-7721), respectively.
已经制备了一系列 2-苄基苯并呋喃和咪唑的新型杂合化合物，并对其进行了体外评估，以对抗一组人类肿瘤细胞系。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 46 和 47 被发现是针对 5 株人类肿瘤细胞系的最有效衍生物，比顺铂（DDP）更有效，并且对乳腺癌（MCF-7）和髓样肝癌（SMMC-7721）具有选择性的细胞毒性活性。
