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ID: ALA1135353
Journal: Bioorg Med Chem Lett
Title: Synthesis and initial SAR studies of 3,6-disubstituted pyrazolo[1,5-a]pyrimidines: a new class of KDR kinase inhibitors.
Authors: Fraley ME, Hoffman WF, Rubino RS, Hungate RW, Tebben AJ, Rutledge RZ, McFall RC, Huckle WR, Kendall RL, Coll KE, Thomas KA.
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.
CiteXplore: 12217372