Synthesis and biological evaluation of new pyrimidine-4-yl-ethanol derivatives as ROS1 kinase inhibitors

摘要

As a part of trials to target ROS1 kinase with potential inhibitors, a novel series of pyrimidin-4-yl-ethanol and ethanone derivatives (4a–f, 5a–f, 6a–f and 7a–f) have been designed based on previously discovered lead compounds KIST301072 and KIST301080, and synthesized on 4–5 steps according to compounds. The structures of the newly synthesized compounds have been confirmed on 1H-NMR, 13C-NMR and IR. Most of the tested compounds showed ROS1 kinase inhibitory activity in micromolar range.