Synthesis and biological evaluation of novel dasatinib analogues as potent DDR 1 and DDR 2 kinase inhibitors

Novel dasatinib analogues as DDR 1 and DDR 2 inhibitors were designed and synthesized. The synthesized compounds were screened for DDR 1 and DDR 2 kinase inhibitory and cancer cell proliferation inhibitory activities. Some of the compounds showed the potent inhibitory activities against both DDR 1 and DDR 2, as well as anticancer activity in low nanomolar range against K562 cell line; especially, compound 3j demonstrated significantly better inhibitory potency than the parental dasatinib against both DDR s and also demonstrated the potent inhibitory activity against K562 cell lines ( IC 50 values of 2.26±0.46 n m for DDR 1, 7.04±2.90 n m for DDR 2, and 0.125±0.017 n m for K562 cell line).