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

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.

journal_name

Bioorg Med Chem

authors

McDermott LA,Simcox M,Higgins B,Nevins T,Kolinsky K,Smith M,Yang H,Li JK,Chen Y,Ke J,Mallalieu N,Egan T,Kolis S,Railkar A,Gerber L,Luk KC

doi

10.1016/j.bmc.2005.05.012

subject

Has Abstract

pub_date

2005-08-15 00:00:00

pages

4835-41

issue

16

eissn

0968-0896

issn

1464-3391

pii

S0968-0896(05)00420-7

journal_volume

13

pub_type

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