Title of article :
Synthesis and Initial SAR Studies of 3,6-Disubstituted Pyrazolo[1,5-a]pyrimidines: A New Class of KDR Kinase Inhibitors
Author/Authors :
Mark E. Fraley، نويسنده , , William F. Hoffman، نويسنده , , Robert S. Rubino، نويسنده , , Randall W. Hungate، نويسنده , , Andrew J. Tebben، نويسنده , , Ruth Z. Rutledge، نويسنده , , Rosemary C. McFall، نويسنده , , William R. Huckle، نويسنده , , Richard L. Kendall، نويسنده , , Kathleen E. Coll، نويسنده , , Kenneth A. Thomas، نويسنده ,
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 IC50=19 nM), respectively. The synthesis and SAR of these compounds are described.
