Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3

  • Bioorg Med Chem Lett. 2006 Jun 15;16(12):3282-6. doi: 10.1016/j.bmcl.2006.03.032.
Raymond J Patch  1 ,  Christian A Baumann ,  Jian Liu ,  Alan C Gibbs ,  Heidi Ott ,  Jennifer Lattanze ,  Mark R Player
Affiliations
  • 1. Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA.
PMID: 16580199 DOI: 10.1016/j.bmcl.2006.03.032
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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