Thienopyridine urea inhibitors of KDR kinase

被引：39
|
作者：
Heyman, H. Robin
Frey, Robin R.
Bousquet, Peter F.
Cunha, George A.
Moskey, Maria D.
Ahmed, Asma A.
Soni, Niru B.
Marcotte, Patrick A.
Pease, Lori J.
Glaser, Keith B.
Yates, Melinda
Bouska, Jennifer J.
Albert, Daniel H.
Black-Schaefer, Candace L.
Dandliker, Peter J.
Stewart, Kent D.
Rafferty, Paul
Davidsen, Steven K.
Michaelides, Michael R.
Curtin, Michael L.
机构：
[1] Abbott Labs, Abbott Pk, IL 60064 USA
[2] Abbott Biores Ctr, Worcester, MA 01605 USA
来源：
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS | 2007年 / 17卷 / 05期
关键词：
KDR kinase; VEGF; thienopyridine; urea;
D O I：
10.1016/j.bmcl.2006.12.015
中图分类号：
R914 [药物化学];
学科分类号：
100701 ;
摘要：
A series of substituted thienopyridine ureas was prepared and evaluated for enzymatic and cellular inhibition of KDR kinase activity. Several of these analogs, such as 2, are potent inhibitors of KDR (< 10 nM) in both enzymatic and cellular assays. Further characterization of inhibitor 2 indicated that this analog possessed excellent in vivo potency (ED50 2.1 mg/kg) as measured in an estradiol-induced mouse uterine edema model. (c) 2006 Elsevier Ltd. All rights reserved.
引用
收藏
页码：1246 / 1249
页数：4
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