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

Meriç Köksal | Zendy; Mine Yarim Yüksel | Zendy; İrem Durmaz | Zendy; Rengül Çetin-Atalay | Zendy

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

Author(s) -

Meriç Köksal,

Mine Yarim Yüksel,

İrem Durmaz,

Rengül Çetin-Atalay

Publication year - 2012

Publication title -

turkish journal of chemistry

Language(s) - English

Resource type - Journals

SCImago Journal Rank - 0.239

H-Index - 46

eISSN - 1303-6130

pISSN - 1300-0527

DOI - 10.3906/kim-1111-5

Subject(s) - chemistry , piperazine , cytotoxicity , substituent , cytotoxic t cell , indole test , stereochemistry , in vitro , colorectal cancer , cell culture , liver cancer , pharmacology , cancer , biochemistry , organic chemistry , medicine , biology , genetics

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 IC50 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. © TÜBITAK

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