Synthesis and cytotoxic activities of novel hybrid 2-phenyl-3-alkylbenzofuran and imidazole/triazole compounds |
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| Authors: | Wen Chen Xiao-Yan Deng Yan Li Li-Juan Yang Wei-Chao Wan Xue-Quan Wang Hong-Bin Zhang Xiao-Dong Yang |
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| Institution: | 1. 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;2. State Key Laboratory for Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Science, Kunming 650204, PR China;3. Key Laboratory of Ethnic Medicine Resource Chemistry, State Ethnic Affairs Commission & Ministry of Education, Yunnan University of Nationalities, Kunming 650031, PR China |
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| Abstract: | 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)). |
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| Keywords: | Hybrid compound Benzofuran Imidazole Triazole Structure–activity relationships |
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