Abstract
In a continuation of and update to our research on the synthesis and biological evaluation of 1,2,4-triazolo[ 1,5-a]quinazolines, this study deals with a new series of their 5-hydrazono-[1,2,4] triazolo[1,5-a]quinazolines (1-19) that was synthesized by the reaction of 5-hydrazino-[1,2,4]triazoloquinazolines with a variety of aryl(hetero)aldehydes. Their cytotoxic effects have been evaluated in vitro in relation to human breast MCF-7, hepatocellular Hep-G2, human cervical HeLa and mouse fibroblast L929 cancer cell lines, using MTT assay. The obtained IC50-values are reported in mu g/mL and mu M, using gemcitabine hydrochloride as a reference drug. The findings revealed that compound 11 had significant cytotoxic effects against all four cell lines. Its IC50 values ranged between 18.7 and 191.4 mu g/mL in relation to gemcitabine hydrochloride (IC50 = 169.6-365.3 mu g/mL). However, 6, 13, 14 and 15 showed remarkable significant effect against MCF-7 cell line and 13 and 15 against L929. Compound 6 was found to exhibit the highest activity against Hela cell line.