Novel 3-substituted N-methylcarbazole-imidazolium salt derivatives: Synthesis and cytotoxic activity.
CHEMICAL BIOLOGY & DRUG DESIGN(2018)
Abstract
A series of novel 3-substituted N-methylcarbazole-imidazolium salt derivatives has been prepared and evaluated in vitro against a panel of tumor cell lines (Hep G-2, Hela and PC12). The results suggest that the presence of substituted 2-methyl-imidazole or imidazole ring and substitution of the imidazolyl-3-position with a naphthylacyl or 4-bromophenacyl group were important for improving cytotoxic activity. Compounds 17, 18, 27, and 28 with 4-bromophenacyl and naphthylacyl groups displayed good activities with IC50 values of 0.09-7.20m against three tumor cell lines investigated and more active than DDP. Compound 35 exhibited cytotoxic activity selectively against Hela cell.
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Key words
cytotoxic activity,imidazolium salts,N-methylcarbazole,structure-activity relationship,synthesis
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