新型 2-苯基-3-烷基苯并呋喃和咪唑/三唑杂合化合物的合成及细胞毒性活性。
Synthesis and cytotoxic activities of novel hybrid 2-phenyl-3-alkylbenzofuran and imidazole/triazole compounds.
机构信息
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.
出版信息
Bioorg Med Chem Lett. 2013 Aug 1;23(15):4297-302. doi: 10.1016/j.bmcl.2013.06.001. Epub 2013 Jun 11.
A series of novel hybrid compounds of 2-phenyl-3-alkylbenzofuran and imidazole or triazole were prepared and evaluated in vitro against a panel of human tumor cell lines. The results suggest that the 2-ethyl-imidazole ring, and substitution of the imidazolyl-3-position with a 2-bromobenzyl or naphthylacyl group, were vital for modulating inhibitory activity. In particular, hybrid compound 31 was found to be the most potent derivative with IC₅₀ values of 0.08-0.55 μM against five strains human tumor cell lines and was found to be more selective against breast carcinoma (MCF-7) and colon carcinoma (SW480) (IC₅₀ values 40.8-fold and 40.1-fold lower than cisplatin (DDP)).
一系列新型 2-苯基-3-烷基苯并呋喃和咪唑或三唑的杂合化合物被制备并在体外对一组人肿瘤细胞系进行了评估。结果表明，2-乙基-咪唑环和咪唑基-3-位取代的 2-溴苄基或萘基酰基对于调节抑制活性至关重要。特别是，杂合化合物 31 被发现是最有效的衍生物，对五种人肿瘤细胞系的 IC₅₀ 值为 0.08-0.55 μM，并且对乳腺癌（MCF-7）和结肠癌（SW480）具有更高的选择性（IC₅₀ 值比顺铂（DDP）低 40.8 倍和 40.1 倍）。
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