4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II

Shenlin Huang; Ronghua Li; Kenneth R LaMontagne; Lee M Greenberger; Peter J Connolly

doi:10.1016/j.bmcl.2011.01.053

4-aminopyrimidine-5-carbaldehyde oximes as potent VEGFR-2 inhibitors. Part II

Bioorg Med Chem Lett. 2011 Mar 15;21(6):1815-8. doi: 10.1016/j.bmcl.2011.01.053. Epub 2011 Jan 21.

Authors

Shenlin Huang¹, Ronghua Li, Kenneth R LaMontagne, Lee M Greenberger, Peter J Connolly

Affiliation

¹ Johnson & Johnson Pharmaceutical Research & Development LLC, Raritan, NJ 08869, USA. shenlinhuang@hotmail.com

PMID: 21316232
DOI: 10.1016/j.bmcl.2011.01.053

Abstract

A series of 4-aminopyrimidine-5-carbaldehyde oxime was discovered to have potent VEGFR-2 inhibitory activity. Described here are the chemistry for analogue synthesis and SAR study results. The PK properties, kinase profiling, and in vivo efficacy study for compound 4b are also discussed.

MeSH terms

Animals
Mice
Oximes / chemistry
Oximes / pharmacology*
Rats
Structure-Activity Relationship
Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*

Substances

Oximes
Vascular Endothelial Growth Factor Receptor-2