Synthesis, Cytotoxicity and Molecular Docking of Some Schiff Bases Derived Quinazolinone Bearing Pyrazoline | ||
| Egyptian Journal of Chemistry | ||
| Article 15, Volume 62, Special Issue (Part 1) Innovation in Chemistry, December 2019, Pages 197-209 PDF (2.3 M) | ||
| Document Type: Original Article | ||
| DOI: 10.21608/ejchem.2019.10116.1666 | ||
| Authors | ||
| Sahar El-Sakka* 1; Mohamed Soliman2; Eman El-Sholkany2 | ||
| 1Chemistry Department, Faculty of Science, Suez University | ||
| 2Chemistry 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. | ||
| Keywords | ||
| Quinazolinone; HePG2; Schiff base; Molecular docking; Azomethines | ||
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