Synthesis and biological activity of new bisbenzofuran-imidazolium salts |
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| Institution: | 1. Key Laboratory of Natural Pharmaceutical and Chemical Biology of Yunnan Province, School of Science, Honghe University, Mengzi, Yunnan 661100, PR China;2. Key Laboratory of Medicinal Chemistry for Natural Resource, Ministry of Education and Yunnan Province, School of Chemical Science and Technology, Yunnan University, Kunming 650091, PR China;3. State Key Laboratory for Phytochemistry and Plant Resources in West China, Kunming Institute of Botany, Chinese Academy of Science, Kunming 650204, PR China;4. Department of Soil and Water Science, University of Florida, 2181 McCarty Hall A, Gainesville, FL 32611-0290, USA |
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| Abstract: | A series of novel bisbenzofuran-imidazolium salts were designed and prepared. The in vitro antitumor activity of these derivatives was evaluated against a panel of human tumor cell lines (A549, HL-60, MCF-7, SMMC-7721 and SW480). Results demonstrated that 2-methyl-benzimidazole ring and substitution of the imidazolyl-3-position with a 4-methoxyphenacyl or 2-naphthylacyl substituent were important for promoting cytotoxic activity. Notably, compound 23 was found to be the most potent compound with IC50 values of 0.64–1.47 μM against five human tumor cell lines, and exhibited higher selectivity to MCF-7 and SW-480 cell lines with IC50 values 15.3-fold and 9.1-fold lower than DDP. |
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| Keywords: | Bisbenzofuran Imidazolium salts Biological evaluation Cytotoxic activity Structure-activity relationships |
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