M. Fraley, W. F. Hoffman, R. Rubino
Oct 7, 2002
Citations
3
Influential Citations
99
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Quality indicators
Journal
Bioorganic & medicinal chemistry letters
Abstract
We have synthesized and evaluated the activity of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines as a new class of KDR kinase inhibitors. Starting with screening lead 1, potency against isolated KDR was fully optimized with 3-thienyl and 4-methoxyphenyl substituents at the 6- and 3-positions (3g, KDR IC(50)=19 nM), respectively. The synthesis and SAR of these compounds are described.