Structure-based design, synthesis and antiproliferative action of new quinazoline-4-one/chalcone hybrids as EGFR inhibitors

Faculty of Pharmacy

Assiut University

Structure-based design, synthesis and antiproliferative action of new quinazoline-4-one/chalcone hybrids as EGFR inhibitors

Research Authors
Mohamed Hisham, Heba A. Hassan, Hesham A. M. Gomaa, Bahaa G.M. Youssif, Alaa M. Hayallah, Mohamed Abdel-Aziz
Research Date
Research Department
Department of Pharmaceutical Organic Chemistry
Research Journal
Journal Molecular Structure
Research Publisher
Science direct
Research Rank
Medicinal Chemistry
Research Vol
1254
Research Year
2022
Research Member
Bahaa Gamal Al-Din Mohammad Yousef
Alaa Arafat Khalifa Mohamed
Research_Pages
132422
Research Abstract

A new series of quinazoline-4-one/chalcone hybrids, 7–26 , was synthesized in this study as EGFR in- hibitors with antiproliferative activity. Target compounds were synthesized and in vitro tested against different cancer cell lines, EGFR, and BRAF enzymes. Three compounds showed the greatest antiprolif- erative activity and were the most potent EGFR inhibitors. Also, these three compounds improved the level of active caspase-3, 8, and 9 with potent induction of cytochrome c and Bax levels, as well as down regulation of Bcl - 2 levels. Finally, the most active inhibitors docked well inside EGFR active sites.