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Published on: June 28, 2021
Design, Synthesis and Antitumor Evaluation of Novel Pyrazolopyrimidines and Pyrazoloquinazolines
Mohamed El-Naggar1, Ashraf S Hassan2, Hanem M Awad3
1Chemistry Department, Faculty of Sciences, University of Sharjah, Sharjah 27272, UAE. M5elnaggar@yahoo.com.
Abstract:
A series of N-aryl-7-aryl-pyrazolo[1,5-a]pyrimidines 18a⁻u and N-aryl-pyrazolo[1,5-a]quinazolines 25a⁻c were designed and synthesized via the reaction of 5-aminopyrazoles 11a⁻c with enaminones 12a⁻g or 19, respectively. The new compounds were screened for their in vitro antitumor activity toward liver (HepG-2) and breast (MCF-7) human cancer cells using 3-[4,5-dimethyl-2-thiazolyl)-2,5-diphenyl-2H-tetrazolium bromide MTT assay. From the results, it was found that all compounds showed dose-dependent cytotoxic activities against both HepG-2 and MCF-7 cells. Two compounds 18o and 18a were selected for further investigations. Cell cycle analysis of liver (HepG-2) cells treated with 18o and breast (MCF-7) cells treated with 18a showed cell cycle arrest at G2/M phase and pro-apoptotic activity as indicated by annexin V-FITC staining.
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