Article
Design, synthesis and biological evaluation of potent epidermal growth factor receptor tyrosine kinase (EGFR-TK) inhibitors against resistance mutation for lung cancer treatment.
Bioorganic chemistry - 1 Feb 2024
Wang Cheng, Wang Xin, Wang Xiaoxue, Tian Baorui, Zhang Sihe, Wang Tianqi, Ma Yakun, Fan Yan
Abstract excerpt
In this study, we identified a newly synthesized compound 7o with potent inhibition on EGFR primary mutants (L858R, Del19) and drug-resistant mutant T790M with nanomolar IC50 values. 7o showed strong antiproliferative effects against EGFR mutant-driven non-small cell lung cancer (NSCLC) cells such as H1975, PC-9 and HCC827, over cells expressing EGFRWT. Molecular docking was performed to investigate the possible...
Topics
- Humans
- Lung Neoplasms
- Carcinoma, Non-Small-Cell Lung
- ErbB Receptors
- Molecular Docking Simulation
- Cell Proliferation
- Protein Kinase Inhibitors
- Mutation
- Cell Line, Tumor
- Drug Resistance, Neoplasm