Document Detail

Synthesis and biological study of 4-aminopyrimidine-5-carboxaldehyde oximes as antiproliferative VEGFR-2 inhibitors.
MedLine Citation:
PMID:  16979339     Owner:  NLM     Status:  MEDLINE    
A novel 4-aminopyrimidine-5-carboxaldehyde oxime scaffold with inhibitory activity against VEGFR-2 kinase has been identified. With a 4-fluoro-2-methylindol-5-yloxy group at the 6-position and alkyl groups as the oxime side chains, many analogues showed good potency for VEGFR-2. This series also exhibited antiproliferative activity against cancer cells, causing cell accumulation at the G2/M phase of the cell cycle and preventing cells from entering mitosis. Described here are the chemistry, structure-activity relationships (SAR), and biological testing for this series.
Shenlin Huang; Ronghua Li; Peter J Connolly; Guozhang Xu; Michael D Gaul; Stuart L Emanuel; Kenneth R Lamontagne; Lee M Greenberger
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Publication Detail:
Type:  Journal Article     Date:  2006-09-18
Journal Detail:
Title:  Bioorganic & medicinal chemistry letters     Volume:  16     ISSN:  0960-894X     ISO Abbreviation:  Bioorg. Med. Chem. Lett.     Publication Date:  2006 Dec 
Date Detail:
Created Date:  2006-11-10     Completed Date:  2007-01-08     Revised Date:  2009-11-19    
Medline Journal Info:
Nlm Unique ID:  9107377     Medline TA:  Bioorg Med Chem Lett     Country:  England    
Other Details:
Languages:  eng     Pagination:  6063-6     Citation Subset:  IM    
Johnson and Johnson Pharmaceutical Research and Development, L.L.C, 1000 Route 202, Raritan, NJ 08869, USA. <>
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MeSH Terms
Cell Proliferation / drug effects
Hela Cells
Molecular Structure
Oximes / chemical synthesis,  chemistry*,  pharmacology*
Protein Kinase Inhibitors / chemical synthesis*,  chemistry,  pharmacology*
Pyrimidines / chemical synthesis*,  pharmacology*
Structure-Activity Relationship
Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*,  metabolism
Reg. No./Substance:
0/Oximes; 0/Protein Kinase Inhibitors; 0/Pyrimidines; EC Endothelial Growth Factor Receptor-2

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