Design, synthesis and evaluation of (E)-α-benzylthio chalcones as novel inhibitors of BCR-ABL kinase

Novel (E)-α-benzylthio chalcones are reported with preliminary in vitro activity data indicating that several of them are potent inhibitors (comparable to imatinib, the reference compound) of BCR-ABL phosphorylation in leukemic K562 cells, known to express high levels of BCR-ABL. The ability of such compounds to significantly inhibit K562 cell proliferation suggests that this scaffold could be a promising lead for the development of anticancer agents that are able to block BCR-ABL phosphorylation in leukemic cells.

The design, synthesis and biological evaluation of novel (E)-α-benzylthio chalcones as BCR-ABL kinase inhibitors are described. The structure–activity relationship, in vitro cytotoxicity in K562, a human leukemic cell line and inhibition of BCR-ABL phosphorylation by these compounds is discussed.Figure optionsDownload as PowerPoint slide