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

DOI

10.3906/kim-1111-5

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

First Page

515

Last Page

525

Recommended Citation

AKKOÇ, MERİÇ KÖKSAL; YÜKSEL, MİNE YARIM; DURMAZ, İREM; and ATALAY, RENGÜL ÇETİN (2012) "Design, synthesis, and biological evaluation of indole-based 1,4-disubstituted piperazines as cytotoxic agents," Turkish Journal of Chemistry: Vol. 36: No. 4, Article 3. https://doi.org/10.3906/kim-1111-5
Available at: https://journals.tubitak.gov.tr/chem/vol36/iss4/3