Conformational Constrained 4‑(1-Sulfonyl-3-indol)yl-2-phenylaminopyrimidine Derivatives as New Fourth-Generation Epidermal Growth Factor Receptor Inhibitors Targeting T790M/C797S Mutations

Tertiary C797S mutation of epidermal growth factor receptor (EGFR)-mediated resistance in non-small-cell-lung-cancer (NSCLC) patients is still an unmet clinical need. Several classes of adenosine 5′-triphosphate-competitive or allosteric EGFRT790M/C797S inhibitors and degraders have been developed,...

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Veröffentlicht in:Journal of medicinal chemistry 2022-05, Vol.65 (9), p.6840-6858
Hauptverfasser: Chen, Hao, Lai, Mengzhen, Zhang, Tao, Chen, Yuqing, Tong, Linjiang, Zhu, Sujie, Zhou, Yang, Ren, Xiaomei, Ding, Jian, Xie, Hua, Lu, Xiaoyun, Ding, Ke
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