Synthesis and cytotoxic activities of novel phenacylimidazolium bromides |
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Authors: | Xiao-Dong Yang Xiang-Hui Zeng Yan-Li Zhang Chen Qing Wen-Jian Song Liang Li Hong-Bin Zhang |
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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. Yunnan Key Laboratory of Pharmacology for Natural Products, Kunming Medical University, Kunming 650031, PR China |
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Abstract: | A series of novel phenacylimidazolium derivatives, bearing an aryl or alkyl substituent at position-1 and a phenacyl substituent at position-3 of the imidazole ring, has been prepared and evaluated in vitro against a panel of human tumor cell lines. Phenacylimidazolium bromides bearing a highly sterically hindered aryl group at position-1 and an electron-rich phenacyl or naphthylacyl substituent at position-3 of imidazole ring proved to be more active than imidazolium bromides with other substituted groups. In particular, compound 5j was found to be the most potent compounds with IC50 values lower than 5.0 μM against 8 strains human tumor cell lines and more active than cisplatin (DDP). |
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