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  • Title: Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
    Author: Patch RJ, Baumann CA, Liu J, Gibbs AC, Ott H, Lattanze J, Player MR.
    Journal: Bioorg Med Chem Lett; 2006 Jun 15; 16(12):3282-6. PubMed ID: 16580199.
    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.
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