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

Document Type: Research article

Authors

1 Novel Drug Delivery Research Center, Faculty of Pharmacy, Kermanshah University of Medical Sciences, Kermanshah, Iran.

2 1- Student’s Research Committee, Kermanshah University of Medical Sciences, Kermanshah, Iran. 2- Medical Biology Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran.

3 Medical Biology Research Center, Kermanshah University of Medical Sciences, Kermanshah, Iran.

4 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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