Insights into the design of inhibitors of the EGFR family with anticancer activity overcoming resistance: A case of optimizing thieno[2,3-d]pyrimidine-based EGFR inhibitors

Journal of Molecular Structure(2022)

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摘要
•Thieno[2,3-d]pyrimidine-based dual EGFR/HER2 inhibitors were designed.•12 compounds were prepared and tested against EGFR, HER2 and T790M/L858R.•Their anti-proliferative activities were assessed against relevant cancer cell lines.
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关键词
Dual EGFR/HER2 inhibitor,EGFR inhibitor resistance,EGFR-T790M/L858R,Thieno[2,3-d]pyrimidine,DFT,Anticancer
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