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RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: synthesis and biological evaluation
Lee A McDermott1, Mary Simcox, Brian Higgins
1Hoffmann-La Roche Inc., 340 Kingsland Str., Nutley, NJ 07110, USA. lee.mcdermott@roche.com
Bioorganic & Medicinal Chemistry
|June 15, 2005
Abstract:
(+/-)-1-(anti-3-Hydroxy-cyclopentyl)-3-(4-methoxy-phenyl)-7-phenylamino-3,4-dihydro-1H-pyrimido[4,5-d]pyrimidin-2-one (RO4383596) is a potent and selective inhibitor of the pro-angiogenic receptor tyrosine kinases KDR, FGFR, and PDGFR. This agent has an excellent pharmacokinetic profile and is highly efficacious in rodent models of angiogenesis upon oral administration.
