960化工网
Design, synthesis and bioactivity evaluation of novel quinazoline based KRASG12C inhibitors†
Qingxu Liu
New Journal of Chemistry Pub Date : 02/07/2022 00:00:00 , DOI:10.1039/D1NJ06226C
Abstract

KRAS is a member of the RAS gene family, which is involved in the regulation of human life activities. KRASG12C mutation is distributed in many tumors and has been the focus of attention. In our study, we analyzed the binding of BAY-293 to KRAS protein using molecular docking technology. We designed and synthesized 20 compounds and tested their bioactivity. At the same time, we found that compound 8P (IC50 = 2.6 ± 1.2 μM) had good inhibitory activity against the A549 cell line and compound 8e had a good inhibitory effect on the McF-7 cell line with IC50 = 5.5 ± 0.3 μM.

Graphical abstract: Design, synthesis and bioactivity evaluation of novel quinazoline based KRASG12C inhibitors
平台客服
平台客服
平台在线客服