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Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFRL858R/T790M/C797S.

Abstract：

:In this paper, we describe the discovery and optimization of a series of noncovalent reversible epidermal growth factor receptor inhibitors of EGFRL858R/T790M/C797S. One of the most promising compounds, 25g, inhibited the enzymatic activity of EGFRL858R/T790M/C797S with an IC50 value of 2.2 nM. Cell proliferation assays showed that 25g effectively and selectively inhibited the growth of EGFRL858R/T790M/C797S-dependent cells. This series of compounds, which occupy both the ATP binding site and the allosteric site of the EGFR kinase, may serve as a basis for the development of fourth-generation EGFR inhibitors for L858R/T790M/C797S mutants.

journal_name

ACS Med Chem Lett

journal_title

ACS medicinal chemistry letters

authors

Li Q,Zhang T,Li S,Tong L,Li J,Su Z,Feng F,Sun D,Tong Y,Wang X,Zhao Z,Zhu L,Ding J,Li H,Xie H,Xu Y

doi

10.1021/acsmedchemlett.8b00564

subject

Has Abstract

pub_date

2019-05-22 00:00:00

pages

869-873

issue

6

issn

1948-5875

journal_volume

10

pub_type

杂志文章

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