Title of article
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3
Author/Authors
Raymond J. Patch، نويسنده , , Christian A. Baumann، نويسنده , , Jian Liu، نويسنده , , Alan C. Gibbs، نويسنده , , Heidi Ott، نويسنده , , Jennifer Lattanze، نويسنده , , Mark R. Player، نويسنده ,
Issue Information
روزنامه با شماره پیاپی سال 2006
Pages
5
From page
3282
To page
3286
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 μM) and blocks the proliferation of MV4-11 cells (IC50 = 0.41 μM). 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.
Keywords
FLT3 , AML , Acute myeloid leukemia , Acylamino-3-carboxamide
Journal title
Bioorganic & Medicinal Chemistry Letters
Serial Year
2006
Journal title
Bioorganic & Medicinal Chemistry Letters
Record number
796974
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