Synthesis, Cytotoxicity and Molecular Docking of Some Schiff Bases Derived Quinazolinone Bearing Pyrazoline

Document Type : Original Article

Authors

1 Chemistry Department, Faculty of Science, Suez University

2 Chemistry Department, Faculty of Science, Suez University, Suez, Egypt

Abstract

A novel quinazolinone derivatives based on 3-amino-2-[3-(4-methoxy-3-methylphenyl)-4,5-dihydro-1H-pyrazol-5-yl]-4(3H)-qunazolinones were designed, synthesized and evaluated for their in vitro cytotoxic activity against the hepatic carcinoma cell line (HepG-2), the results revealed that the tested compounds process inhibitory effects on the growth of HepG2 liver cancer cells. 3-amino-2-[3-(4-methoxy-3-methylphenyl)-4,5-dihydro-1H-pyrazol-5-yl]-4(3H)-quinazolinone showed the highest inhibition activity against HepG2 cell line (IC50 equals 67.8 µg/ml) among the tested compounds. The molecular modelling studies were performed to explore the detailed binding affinity towards the human liver carcinoma HepG2. The obtained results proved that the most active 3-amino-2-[3-(4-methoxy-3-methylphenyl)-4,5-dihydro-1H-pyrazol-5-yl]-4(3H)-quinazolinone could be useful as a template for future design, adaptation and investigation to construct more active qunazolinone analogs. Moreover, compounds were screened for antibacterial activity and none of them showed noteworthy activity.

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History

  • Receive Date: 01 March 2019
  • Revise Date: 21 April 2019
  • Accept Date: 25 June 2019

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