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Cell cycle inhibition, apoptosis, and molecular docking studies of the novel anticancer bioactive 1,2,4-triazole derivatives

  • Javad Ghanaat
  • Mohammad A. KhalilzadehEmail author
  • Daryoush Zareyee
  • Mohammadreza Shokouhimehr
  • Rajender S. Varma
Original Research
First Online:
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Abstract

Several 3-alkylsulfanyl-1,2,4-triazole derivatives were synthesized and their relevant structures confirmed based on their elemental analysis and nuclear magnetic resonance. The anticancer activity of all the derivatives was evaluated for A549, MCF7, and SKOV3 cell lines by the 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyl tetrazolium bromide assay wherein compound 5e demonstrated significant anti-proliferative activities against all cell lines whereas 5b and 5e showed efficient anti-proliferative actions in SKOV3 cell line having half maximal inhibitory concentration (IC50) values of 0.81 and 0.53 μM, respectively. Furthermore, compound 5e was found to drive remarkable cell cycle arrest at the G2/M phase for SKOV3 cell lines in a concentration-dependent behavior. Molecular docking studies performed with these derivatives validated them as appropriate candidates for further studies of their potential anticancer activity.

Keywords

1,2,4-Triazoles Anticancer activity Molecular docking Anticancer agents 
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Notes

Compliance with ethical standards

Conflict of interest

The authors declare that they have no conflict of interest.

Ethical approval

This article does not contain any studies with human participants or animals performed by any of the authors.

Supplementary material

11224_2019_1453_MOESM1_ESM.docx (1.7 mb)
ESM 1 (DOCX 1779 kb)

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© Springer Science+Business Media, LLC, part of Springer Nature 2019

Authors and Affiliations

  1. 1.Department of Chemistry, Qaemshahr BranchIslamic Azad UniversityQaemshahrIran
  2. 2.Department of Materials Science and Engineering, Research Institute of Advanced MaterialsSeoul National UniversitySeoulRepublic of Korea
  3. 3.Regional Centre of Advanced Technologies and Materials, Faculty of SciencePalacky University in OlomoucOlomoucCzech Republic

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