RO4383596, an orally active KDR, FGFR, and PDGFR inhibitor: Synthesis and biological evaluation

Lee A. McDermott, Mary Simcox, Brian Higgins, Tom Nevins, Kenneth Kolinsky, Melissa Smith, Hong Yang, Jia K. Li, Yingsi Chen, June Ke, Navita Mallalieu, Tom Egan, Stan Kolis, Aruna Railkar, Louise Gerber, Kin Chun Luk

Research output: Contribution to journalArticlepeer-review

24 Scopus citations

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.

Original languageEnglish
Pages (from-to)4835-4841
Number of pages7
JournalBioorganic and Medicinal Chemistry
Volume13
Issue number16
DOIs
StatePublished - 15 Aug 2005
Externally publishedYes

Keywords

  • FGFR inhibitor
  • KDR inhibitor
  • PDGFR inhibitor
  • Pyrimidopyrimidone
  • RO4383596
  • VEGFR inhibitor

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