Synthesis, characterization and cytotoxicity evaluation of 5-hydrazono-[1,2,4]triazolo[1,5-a]quinazolines (Part I).

Journal Article

Marzouk., Rashad Al-Salahi, Elsayed A. Elsayed, Rabab A. El Dib, Mohammad Wadaan, Esam Ezzeldin & Mohamed . 2016

• المجلة \ الصحيفة: Lat. Am. J. Pharm
• رقم العدد: 1
• رقم الإصدار السنوي: 35
• الصفحات: 58-65

مستخلص المنشور

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 μg/mL and μM, 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 μg/mL in relation to gemcitabine hydrochloride (IC50 = 169.6–365.3 μg/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.