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

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.

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

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.
Turkish Journal of Chemistry-Cover
  • ISSN: 1300-0527
  • Yayın Aralığı: 6
  • Yayıncı: TÜBİTAK
Sayıdaki Diğer Makaleler

Symmetric, twinned, and double-decker phthalocyanines substituted by trialkylated pentaerythritol

Muzaffer KÖÇ, Ayşe Gül GÜREK, Fabienne DUMOULİN, Vefa AHSEN

Microwave-assisted synthesis, spectroscopy, and crystal structures of [(H2-(4,4'-bipy)]2+ [Cr2O7]2- and one-dimensional polymeric {[Mn(4,4'-bipy)(Cr2O7)(H2O)2]\}n compounds

Hirihattaya PHETMUNG, Munee WATEH, Chaveng PAKAWATCHAI

Simultaneous determination of dopamine, uric acid, and tryptophan using an MWCNT modified carbon paste electrode by square wave voltammetry

Hadi BEITOLLAHI, Alireza MOHADESI, Saeedeh KHALILIZADEH MAHANI

Three-component Passerini-Smiles coupling reaction of aldehydes and isocyanides with tropolone catalyzed by silica nanoparticles

Abdolhossain MASSOUDI, Issa AMINI, Ali RAMAZANI And

A new absorption based CO2 sensor based on Schiff base doped ethyl cellulose

Sevinç Zehra TOPAL, Kadriye ERTEKİIN, Berrin YENİIGÜL, Ayşe ERÇAĞ

Facile and rapid synthesis of some novel polysubstituted imidazoles by employing magnetic Fe3O4 nanoparticles as a high efficient catalyst

Bahador KARAMI, Khalil ESKANDARI, Abdolmohammad GHASEMI

Titrimetric determination of anionic surfactant content in anionic/nonionic surfactant mixture solution by anionic surfactant selective electrode

Junwei WANG, Zhiping DU, Wanxu WANG, Wei XUE

Synthesis and structural characterization of novel square pyramidal oxovanadium(IV) complexes with ligands having N and O donor atoms

Ashok Kumar YADAVA, Hardeo Singh YADAV, Uma Shanker YADAV

Determination of lidocaine based on electrocatalysis of a chemically modified electrode

Gamze TAN, Gülçin BOLAT, Mehmet Ali ONUR, Serdar ABACI

Microwave-assisted synthesis, spectroscopy, and crystal structures of $[(H_2 -(4,4'-bipy)]^{2+} [Cr_2O_7]^{2−}$ and one-dimensional polymeric ${[Mn(4,4' -bipy)(Cr_2O_7)(H_2O)_2]}_n$ compounds

Hirihattaya PHETMUNG, Munee WATEH, Chaveng PAKAWATCHAI