Epidermal growth factor receptor (EGFR) is one of the important and valuable drug targets. Overexpression of EGFR is associated with the development of many types of cancer. In this study, three PROTACs small molecules (16a-16c) were designed, synthesized and evaluated for their cytotoxicity against the growth in different NSCLC cell line and the degradation effect. The bioassay results indicated that 16c has a good inhibition in PC9 cells and H1975 cells, and the corresponding IC50 value was 0.413 μM and 0.657 μM, respectively. Western blotting results demonstrated that compound 16c could serve as an effective EGFRdel19-targeting degrader in PC9 cells.

中文翻译：

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发现和针对以奥美替尼和来那度胺为基础的EGFR降解剂的针对嵌合体（PROTAC）的蛋白水解生物评估。

表皮生长因子受体（EGFR）是重要且有价值的药物靶标之一。EGFR的过表达与多种类型癌症的发展有关。在这项研究中，设计，合成和评估了三个PROTAC小分子（16a-16c）对不同NSCLC细胞系中的生长的细胞毒性和降解效果。生物测定结果表明，16c在PC9细胞和H1975细胞中具有良好的抑制作用，相应的IC50值分别为0.413μM和0.657μM。蛋白质印迹结果表明，化合物16c可以作为PC9细胞中靶向EGFRdel19的有效降解剂。