Design and Synthesis of New Sulfonamides-Based Flt3 Inhibitors
2019
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, quizatrinib and F6M, were used to guide 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.
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