- Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
Bioorganic & medicinal chemistry letters (2006-04-04)
Raymond J Patch, Christian A Baumann, Jian Liu, Alan C Gibbs, Heidi Ott, Jennifer Lattanze, Mark R Player
PMID16580199
RESUMEN
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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2-(3,4-Dimethoxy-benzoylamino)-4,5,6,7-tetrahydro-benzo[b]thiophene-3-carboxylic acid amide, ≥98% (HPLC), solid