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Peer-reviewed veterinary case report

Thienopyridine urea inhibitors of KDR kinase.

Journal:
Bioorganic & medicinal chemistry letters
Year:
2007
Authors:
Heyman, H Robin et al.
Affiliation:
Global Pharmaceutical Research and Development · United States

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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Original publication: https://pubmed.ncbi.nlm.nih.gov/17188869/