Synthesis, and In-vitro Cytotoxicity Studies of a Series of Triazene Derivatives on Human Cancer Cell Lines

Authors

  • Ali Mostafaie Medical Biology Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran.
  • Hadi Adibi Novel Drug Delivery Research Center, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.
  • Kamran Mansouri Medical Biology Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran.
  • Mohammad Bagher Majnooni 1- Student’s Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran. 2- Medical Biology Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran.
  • Moslem Mohammadi Analytical Chemistry Department, Faculty of Chemistry, Razi University, Kermanshah, Iran.
Abstract:

Compounds containing triazene ring structure are cytotoxic agents and clinically used as antitumor alkylating agents. In this study, a series of triazene derivatives holding alkyl and aryl moieties were synthesized and proved to be potent cytotoxic agents in-vitro particularly against eight cancer cell lines (PC3, HT29, Hela, HL60, Jurkat, K562, MCF7, HepG2) and a non-cancerous cell line (HUVEC). The cytotoxic activity was assessed using two methods, LDH assay, and trypan blue exclusion. Some of the triazene derivatives showed cytotoxic activity more than temozolomide (TMZ) as the reference drug. The synthesized triazenes showed marked cytotoxicity effects on all eight cancer cell lines. Among the compounds synthesized, 1,3-bis(2-ethoxyphenyl)triazene C had unique efficacy and selectivity so that it had IC50 between 0.560-3.33 µM on cancer cell lines and 12.61 μM on normal cell line (HUVEC). 1-(4-nitrophenyl)-3-(2-hydroxyethyl)triazene E shows weaker effect on cancer cell lines than the other compounds having IC50 between 3-15.54 μM.

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Journal title

volume 12  issue 4

pages  695- 703

publication date 2013-11-01

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