Design and Synthesis of Novel EGFR Inhibitors with L-Rhamnose-Benzoxazinone Hybrids

作者:Zhang, Renshuai; Chen, Shaopeng; Wu, Guanzhao; Wan, Shengbiao; Jiang, Tao*
来源:Journal of Heterocyclic Chemistry, 2016, 53(5): 1563-1569.
DOI:10.1002/jhet.2463

摘要

Four L-rhamnose-benzoxazinone compounds as epidermal growth factor receptor (EGFR) tyrosine kinase inhibitors were designed and synthesized. All structures of the compounds were characterized by H-1-NMR, C-13-NMR, and high-resolution mass spectrometry. The inhibition activities of the target compounds for the EGFR tyrosine kinase activity in vitro were determined. Compounds 6a-d displayed moderate activity in targeting EGFR.