Design, synthesis, and biological evaluation of indole-based 1,4-disubstituted piperazines as cytotoxic agents

Authors: MERİÇ KÖKSAL AKKOÇ, MİNE YARIM YÜKSEL, İREM DURMAZ, RENGÜL ÇETİN ATALAY

Abstract: A series of 3-[(4-substitutedpiperazin-1-yl)methyl]-1H-indole derivatives were synthesized, and their structures were confirmed by spectral analysis. All the compounds were tested for their cytotoxic activity in vitro against 3 human tumor cell lines: human liver (HUH7), breast (MCF7), and colon (HCT116). Among the designed derivatives, most of the compounds showed significant cytotoxicity against liver and colon cancer cell lines with lower IC_{50} concentrations than the standard drug 5-fluorouracil. Compound 3s, with 3,4-dichlorophenyl substituent on the piperazine ring, was the most active in suppressing the growth of all screened cancer cells.

Keywords: Anticancer activity, cytotoxicity, Mannich base, indole, 1,4-substituted piperazines

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