Abstract
Aim: To synthesize new analogues of ponatinib and evaluate anti-leukemia cells and cytotoxicity. Methodology & results: The inhibitory activity of compounds 13a and 13c against K562 and HL60 cells was comparable to that of ponatinib (IC50=0.74, 0.88 vs 0.64nM and 0.59, 0.77 vs 0.39nM, respectively). Compounds 13a and 40b were 34-and 77-fold more potent than ponatinib against KG1a cells (IC50=0.091 and 0040 vs 3.6μM, respectively). Compounds 13a, 13c and 40b also decreased the Abl protein level in the K562 cells, inhibited colony formation in MCF-7 cells and inhibited cell migration in B16BL6 cells. Compound 13a showed low cytotoxicity in 293 cells. Conclusion: Compound 13a was the best lead compound.
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