Design and Synthesis of New Sulfonamides–Based Flt3 Inhibitors

(E-pub Ahead of Print)

Author(s): Reem Fawaz Abutayeh, Jehad Almaliti, Mutasem O. Taha*.

Journal Name: Medicinal Chemistry

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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.

Keywords: Flt3, Quizatrinib, F6M, Sulfonamides, VEGFR2.

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Article Details

(E-pub Ahead of Print)
DOI: 10.2174/1573406415666190401144053
Price: $95

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