Synthesis and primary cytotoxicity evaluation of new diaryltriazenes

摘要

A series of triazenes derived from 5-(4-aminophenyl)-2,4-dihydro-4-substituted-3H-1,2,4-triazole-3-thiones 1a-c,aminoglutethimide or para-aminobenzoic acid have been synthesized for in vitro anticancer properties against three cell lines.The selected compounds;1,3-bis[4(4-methyl-2,4-dihydro-3H-1,2,4-triazole-3-thioxo-5-yl)phenyl]-3H-triazene 2a,1,3-bis[4(4-ethyl-2,4-dihydro-3H-1,2,4-triazole-3-thioxo-5-yl)phenyl]-3H-triazene 2b,1,3-bis[4(4-allyl-2,4- dihydro- 3H-1,2,4- triazole- 3- thioxo- 5- yl) phenyl]- 3H- triazene 2c and 1-[(4-carboxy)phenyl]-3-[4(4-allyl-2,4-dihydro-3H-1,2,4-triazole-3-thioxo-5-yl)phenyl]-3Htriazene 4 show significant activity but not l,3-bis[4-(3-ethyl-2,6-dioxo-3-piperidnyl)phenyl]-3H-triazene 3.2a-c and 4 that pass the criteria for activity in this assay have been scheduled automatically for evaluation against the full panel of 60 human tumour cell lines from leukemia,melanoma,lung,colon,kidney,ovary,breast,prostate and central nervous system cancer at a minimum of five concentrations at 10-fold dilutions.Sulphorhodamine B (SRB) protein assay has been used to estimate cell viability or growth.Compounds 2a-c and 4 show variable antitumor activity against most of the tested sub-panel tumor cell lines.The log10GI50 values of these compounds are comparable to values of dacarbazine and mitozolamide based anticancer agents.