鉴定2-酰氨基噻吩-3-甲酰胺为FLT3的有效抑制剂。
Identification of 2-acylaminothiophene-3-carboxamides as potent inhibitors of FLT3.
作者信息
Patch Raymond J, Baumann Christian A, Liu Jian, Gibbs Alan C, Ott Heidi, Lattanze Jennifer, Player Mark R
机构信息
Drug Discovery, Johnson & Johnson Pharmaceutical Research and Development, L.L.C., 8 Clarke Drive, Cranbury, NJ 08512, USA.
出版信息
Bioorg Med Chem Lett. 2006 Jun 15;16(12):3282-6. doi: 10.1016/j.bmcl.2006.03.032. Epub 2006 Mar 31.
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.
已鉴定出一系列2-酰基氨基噻吩-3-甲酰胺，它们对FLT3酪氨酸激酶表现出强效抑制活性。化合物44抑制分离的酶（IC50 = 0.027微摩尔）并阻断MV4-11细胞的增殖（IC50 = 0.41微摩尔）。在该酶ATP结合位点的拟议结合模型背景下描述了该系列内的构效关系研究。
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