Design, synthesis and bioactivity evaluation of novel quinazoline based KRASG12C inhibitors

被引：2

作者：

Liu, Qingxu ^{[1
]}

Li, Yan ^{[1
,2
,3
]}

Zhi, Ying ^{[1
,2
,3
]}

Liu, Bo ^{[1
,2
,3
]}

Sun, Jingyong ^{[1
,2
,3
]}

机构：

[1] Shandong First Med Univ & Shandong Acad Med Sci, Inst Mat Med, Jinan 250117, Peoples R China

[2] Minist Hlth, Key Lab Biotech Drugs, Jinan 250117, Peoples R China

[3] Key Lab Rare & Uncommon Dis Shandong Prov, Jinan 250117, Peoples R China

来源：

NEW JOURNAL OF CHEMISTRY | 2022年 / 46卷 / 10期

关键词：

PATHWAY;

D O I：

10.1039/d1nj06226c

中图分类号：

O6 [化学];

学科分类号：

0703 ;

摘要：

KRAS is a member of the RAS gene family, which is involved in the regulation of human Life activities. KRAS(G12C) 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 mu M) 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 mu M.

引用

页码：4827 / 4836

页数：10

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