A　series　of　4-((pyrazolo[1,5-a]pyrimidin-6-yl)-1H-pyrazol-1-yl)phenyl-3-benzamide　derivatives　and　4-((imidazo[1,2-b]pyridazin-3-yl)-1H-pyrazol-1-yl-)phenyl-3-benzamide　derivatives　were　designed,　synthesized　as　new　BCR-ABL　tyrosine　kinase　inhibitors　by　using　combinational　strategies　of　scaffold　hopping　and　conformational　constraint.　These　new　compounds　were　screened　for　BCR-ABL1　kinase　inhibitory　activity,　and　most　of　them　appeared　good　inhibitory　activity　against　BCR-ABL1　kinase.　One　of　the　most　potent　compounds　16a　strongly　suppressed　BCR-ABL1　kinase　with　IC50　value　of　8.5　nM.　The　tested　compounds　16a　and　16i　showed　strong　inhibitory　activities　against　K562　with　IC50　value　of　less　than　2　nM.　Molecular　docking　studies　indicated　that　these　compounds　fitted　well　with　the　active　site　of　BCR-ABL1　protein.　The　results　showed　these　inhibitors　may　serve　as　lead　compounds　for　further　developing　new　drugs　targeted　BCR-ABL　kinase.　(C)　2016　Elsevier　Ltd.　All　rights　reserved.