Novel 3-substituted N-methylcarbazole–imidazolium salt derivatives: Synthesis and cytotoxic activity

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 0.09–7.20 μM against three tumor cell lines investigated and more active than DDP. Compound 35 exhibited cytotoxic activity selectively against Hela cell.

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A series of novel 3-substituted N-methylcarbazole–imidazolium salt derivatives were synthesized and their cytotoxic structure-activity relationship studies were reported. Compounds 17, 18 and 28 displayed good activities with IC₅₀ values of 0.09–7.20 μM against three tumor cell lines investigated. Compound 35 exhibited cytotoxic activity selectively against Hela cell.

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