2. Academic Validation
  3. Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors

Synthesis and biological evaluation of new series of quinazoline derivatives as EGFR/HER2 dual-target inhibitors

  • Bioorg Med Chem Lett. 2022 Jul 1:67:128703. doi: 10.1016/j.bmcl.2022.128703.
Xiaoyu Jiao 1,  Qing Zhang 1,  Yue Zhang 1,  Junlan Shao 1,  Lei Ding 1,  Chunlei Tang 2,  Bainian Feng 3
Affiliations

Affiliations

  • 1 School of Pharmaceutical Science, Jiangnan University, Wuxi, China.
  • 2 School of Pharmaceutical Science, Jiangnan University, Wuxi, China. Electronic address: tangcl@jiangnan.edu.cn.
  • 3 School of Pharmaceutical Science, Jiangnan University, Wuxi, China. Electronic address: fengbainian@jiangnan.edu.cn.
PMID: 35364239 DOI: 10.1016/j.bmcl.2022.128703
Abstract

It is generally believed that EGFR/HER2 dual-target inhibitors may overcome the resistance of EGFR TKIs caused by HER2 overexpression. The structure-based synthesis and biological evaluation of quinazoline derivatives as EGFR/HER2 dual-target inhibitors has been studied in this paper. II-1, II-2, III-3, III-4 displayed comparable inhibitory potency against EGFR and HER2 and II-1 showed remarkable antiproliferative activities against NCI-H358/PC-9/Calu-3/NCI-H1781 (EGFR IC50 = 0.30 nM, HER2 IC50 = 6.07 nM, NCI-H358 GI50 = 23.30 nM, PC-9 GI50 = 1.95 nM, Calu-3 GI50 = 23.13 nM NCI-H1781 GI50 = 41.61 nM).

Keywords

Drug resistance; EGFR/HER2 Dual-target inhibitors; Quinazoline.

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