1.
Chem Biodivers
; 19(6): e202200189, 2022 Jun.
Artículo
en Inglés
| MEDLINE
| ID: mdl-35510593
RESUMEN
A series of novel quinazolinone hydrazide derivatives were designed and synthesized as EGFR inhibitors. The results indicated that most of the aimed compounds had potential anti-tumor cell proliferation and EGFR inhibitory activities. In the comprehensive analysis of all the tested compounds, the target compound 9c showed the best anti-tumor cell proliferation activity, (IC50 =1.31â µM for MCF-7, IC50 =1.89â µM for HepG2, IC50 =2.10â µM for SGC), and IC50 =0.59â µM for the EGFR inhibitory activity. Docking results showed that compound 9c could ideally insert the active site and interact with the critical amino acid residues (Val702, Lys721, Met769, Asp831) in the active site.