Identification of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors

…, DJ Osterling, SZ Doktor, DH Albert, JJ Bouska…

Index: Dai, Yujia; Hartandi, Kresna; Soni, Niru B.; Pease, Lori J.; Reuter, David R.; Olson, Amanda M.; Osterling, Donald J.; Doktor, Stella Z.; Albert, Daniel H.; Bouska, Jennifer J.; Glaser, Keith B.; Marcotte, Patrick A.; Stewart, Kent D.; Davidsen, Steven K.; Michaelides, Michael R. Bioorganic and Medicinal Chemistry Letters, 2008 , vol. 18, # 1 p. 386 - 390

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Citation Number: 40

Abstract

Tumor angiogenesis is mediated by KDR and other VEGFR and PDGFR kinases. Their inhibition presents an attractive approach for developing anticancer therapeutics. Here, we report a series of aminopyrazolopyridine ureas as potent VEGFR/PDGFR multitargeted kinase inhibitors. A number of compounds have been identified to be orally bioavailable and efficacious in the mouse edema model.