Insights into the Overcoming EGFRDel19/T790M/C797S Mutation: A Perspective on the 2-Aryl-4-aminothienopyrimidine Backbone,ChemMedChem

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Insights into the Overcoming EGFRDel19/T790M/C797S Mutation: A Perspective on the 2-Aryl-4-aminothienopyrimidine Backbone
ChemMedChem ( IF 3.6 ) Pub Date : 2024-02-14 , DOI: 10.1002/cmdc.202300634
Xuan Zhang ₁ , Jie He ₁ , Shidi Xu ₁ , Li Fu ₁ , Pengwu Zheng ₁ , Shan Xu ₁ , Qingshan Pan ₁ , Wufu Zhu ₁

Affiliation

We modified the traditional 2-aryl-4-aminoquinazoline structure of fourth-generation EGFR inhibitors. As a result, we were able to create a number of novel 2-aryl-4-aminothienopyrimidine derivatives (A1–A45), as well as identify key sites that affect the backbone′s bioactivity but were not previously explored. These sites could be used as references by future researchers.

中文翻译：

深入了解克服 EGFRDel19/T790M/C797S 突变：2-芳基-4-氨基噻吩并嘧啶主链的视角

我们对第四代EGFR抑制剂传统的2-芳基-4-氨基喹唑啉结构进行了修饰。因此，我们能够创造出许多新型 2-芳基-4-氨基噻吩并嘧啶衍生物 ( A1–A45 )，并确定了影响主链生物活性但之前未探索过的关键位点。这些网站可以作为未来研究人员的参考。

更新日期：2024-02-14

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