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

OBJECTIVE of our work based on the synthesis of the quinazolinone derivative, 3-amino2-[3-(4-methoxy-3-methylphenyl)-4,5-dihydro-1H-pyrazol-5-yl]-4(3H)-qunazolinones, and evaluated for cell line. 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 (HepG2), 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 mu g/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.