| Article ID | Journal | Published Year | Pages | File Type |
|---|---|---|---|---|
| 5158890 | European Journal of Medicinal Chemistry | 2017 | 29 Pages |
Abstract
Structural optimization of pyrido[2,3-d]pyrimidin-7-ones yielded new selective EGFRT790M inhibitors. Compound 9s exhibited good pharmacokinetic properties with F value of 16%, and inhibited EGFRL858R/T790M kinase and H1975Â cells with IC50 values of 2.0 and 40Â nM, respectively.191
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Physical Sciences and Engineering
Chemistry
Organic Chemistry
![A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties](/preview/png/5158890.png "First Page Preview: A structure-guided optimization of pyrido[2,3-d]pyrimidin-7-ones as selective inhibitors of EGFRL858R/T790M mutant with improved pharmacokinetic properties")
Authors
Lei Yu, Minhao Huang, Tianfeng Xu, Linjiang Tong, Xiao-e Yan, Zhang Zhang, Yong Xu, Caihong Yun, Hua Xie, Ke Ding, Xiaoyun Lu,