Background: Flt3 is an oncogenic kinase involved in different leukemias. It is most
prominently associated with acute myeloid leukemia (AML). Flt3-specific inhibitors have shown
promising results in interfering with AML.
Methods: The crystallographic structures of two inhibitors complexed within Flt3, namely, quizartinib
and F6M, were used to guide the synthesis of new sulfonamide-based Flt3 inhibitors.
Results: One of the prepared compounds showed low micromolar anti-Flt3 bioactivity, and interestingly,
low micromolar bioactivity against the related oncogenic kinase VEGFR2.