Synthesis and Anti-K562 Cell Activity of Amino Thiazole (Oxazole) Compounds

OBJECTIVE To design and synthesis of a series of dasatinib analogues and their impact on human chronic myelogenous leukemia cell line K562 in vitro. METHODS A new derivative was designed with dasatinib as the lead compound. The target compounds were synthesized by nucleophilic substitution and cyclization. The structure of all the newly synthesized compounds were identified by ¹H-NMR, ¹³C-NMR, IR and MS. RESULTS Five compounds (10a, 10b. 10c, 10f, 10g) showed higher effective antitumor activity than imatinib; four compounds (10a, 10b, 10C, 10f) exhibited more potent inhibitor versus the K562 cell line compared with the lead compound dasatinib. CONCLUSION The activity can be improved by replacing aromatic benzene ring with quaternary thiazole ring without any change of pharmacophore.