Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3 |
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| Authors: | Patch Raymond J Baumann Christian A Liu Jian Gibbs Alan C Ott Heidi Lattanze Jennifer Player Mark R |
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| Institution: | Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA. |
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| 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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