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ID: ALA1147807

Journal: Bioorg Med Chem Lett

Title: Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.

Authors: Patch RJ, Baumann CA, Liu J, Gibbs AC, Ott H, Lattanze J, Player MR.

Abstract: A series of 2-acylaminothiophene-3-carboxamides has been identified which exhibit potent inhibitory activity against the FLT3 tyrosine kinase. Compound 44 inhibits the isolated enzyme (IC50 = 0.027 microM) and blocks the proliferation of MV4-11 cells (IC50 = 0.41 microM). Structure-activity relationship studies within this series are described in the context of a proposed binding model within the ATP binding site of the enzyme.

CiteXplore: 16580199

DOI: 10.1016/j.bmcl.2006.03.032