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Article

A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties.

European journal of medicinal chemistry - 27 Jan 2017

Yu Lei, Huang Minhao, Xu Tianfeng, Tong Linjiang, Yan Xiao-E, Zhang Zhang, Xu Yong, Yun Caihong, Xie Hua, Ding Ke, Lu Xiaoyun

Abstract excerpt

Structural optimization of pyrido[2,3-d]pyrimidin-7-ones was conducted to yield a series of new selective EGFRT790M inhibitors with improved pharmacokinetic properties. One of the most promising compound 9s potently suppressed EGFRL858R/T790M kinase and inhibited the proliferation of H1975 cells with IC50 values of 2.0 nM and 40 nM, respectively. The compound dose-dependently induced reduction of the...

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Identifiers

PMID: 28033579
DOI: 10.1016/j.ejmech.2016.12.006

Genes

EGFR

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