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

Research paper by Raymond J RJ Patch, Christian A CA Baumann, Jian J Liu, Alan C AC Gibbs, Heidi H Ott, Jennifer J Lattanze, Mark R MR Player

Indexed on: 04 Apr '06Published on: 04 Apr '06Published in: Bioorganic & Medicinal Chemistry Letters


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.