101004-95-9Relevant articles and documents
Discovery of Potent and Noncovalent Reversible EGFR Kinase Inhibitors of EGFRL858R/T790M/C797S
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
supporting information, p. 869 - 873 (2019/06/08)
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.
Synthesis of the 5H-Pyrroloisoindole Ring with 1,3-Dipolar Cycloaddition Reactions
New, J. S.,Yevich, J. P.
, p. 1355 - 1360 (2007/10/02)
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