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. 2007 Mar 1;17(5):1246-9.
doi: 10.1016/j.bmcl.2006.12.015. Epub 2006 Dec 9.

Thienopyridine urea inhibitors of KDR kinase

H Robin Heyman  1 , Robin R Frey, Peter F Bousquet, George A Cunha, Maria D Moskey, Asma A Ahmed, Niru B Soni, Patrick A Marcotte, Lori J Pease, Keith B Glaser, Melinda Yates, Jennifer J Bouska, Daniel H Albert, Candace L Black-Schaefer, Peter J Dandliker, Kent D Stewart, Paul Rafferty, Steven K Davidsen, Michael R Michaelides, Michael L Curtin
Affiliations

Thienopyridine urea inhibitors of KDR kinase

H Robin Heyman et al. Bioorg Med Chem Lett. .

Abstract

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.

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