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Design and Synthesis of New Sulfonamides–Based Flt3 Inhibitors

Author(s):

Reem Fawaz Abutayeh, Jehad Almaliti and Mutasem O. Taha*  

Abstract:


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.

Keywords:

Flt3, Quizatrinib, F6M, Sulfonamides, VEGFR2.

Affiliation:

Department of Pharmaceutical Chemistry and Pharmacognosy, Faculty of Pharmacy, Applied Science Private University, Amman, Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Jordan, Amman, Department of Pharmaceutical Sciences, Faculty of Pharmacy, University of Jordan, Amman



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