- Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFRL858R/T790M/C797S
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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.
- Li, Qiannan,Zhang, Tao,Li, Shiliang,Tong, Linjiang,Li, Junyu,Su, Zhicheng,Feng, Fang,Sun, Deheng,Tong, Yi,Wang, Xia,Zhao, Zhenjiang,Zhu, Lili,Ding, Jian,Li, Honglin,Xie, Hua,Xu, Yufang
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supporting information
p. 869 - 873
(2019/06/08)
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- A Simple One-step Synthesis of N-Substituted Isoindolin-1-ones. Diastereofacially Selective Protonation of an Intermediate Isoindolinol
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α-Amino acids and their methyl esters, arylamines, heterocyclic amines and, less efficiently, aryl substituted aliphatic amines, react with o-phthaldialdehyde in the presence of acetic acid to give N-substituted isoindolin-1-ones in excellent yield; deute
- Grigg, Ronald,Gunaratne, H. Q. Nimal,Sridharan, Visuvanathar
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p. 1183 - 1184
(2007/10/02)
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- Synthesis of the 5H-Pyrroloisoindole Ring with 1,3-Dipolar Cycloaddition Reactions
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The 1,3-dipolar cycloaddition reaction between mesoionic oxazolines, formed from either 1,3-dihydro-2-substituted-2H-isoindole-1-carboxylic acids or 1,3-dihydro-1-oxo-α-substituted-2H-isoindole-2-acetic acids, and dimethylacetylene dicarboxylate has led t
- New, J. S.,Yevich, J. P.
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p. 1355 - 1360
(2007/10/02)
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