Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR

Zhicai Wu; Mark E Fraley; Mark T Bilodeau; Mildred L Kaufman; Edward S Tasber; Adrienne E Balitza; George D Hartman; Kathleen E Coll; Keith Rickert; Jennifer Shipman; Bin Shi; Laura Sepp-Lorenzino; Kenneth A Thomas

doi:10.1016/j.bmcl.2003.12.007

Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR

Bioorg Med Chem Lett. 2004 Feb 23;14(4):909-12. doi: 10.1016/j.bmcl.2003.12.007.

Authors

Zhicai Wu¹, Mark E Fraley, Mark T Bilodeau, Mildred L Kaufman, Edward S Tasber, Adrienne E Balitza, George D Hartman, Kathleen E Coll, Keith Rickert, Jennifer Shipman, Bin Shi, Laura Sepp-Lorenzino, Kenneth A Thomas

Affiliation

¹ Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. [email protected]

PMID: 15012992
DOI: 10.1016/j.bmcl.2003.12.007

Abstract

3,7-Diarylsubstituted imidazopyridines were designed and developed as a new class of KDR kinase inhibitors. A variety of imidazopyridines were synthesized and potent inhibitors of KDR kinase activity were identified with good aqueous solubility.

MeSH terms

Drug Design
Enzyme Inhibitors / chemical synthesis*
Enzyme Inhibitors / pharmacology*
Humans
Molecular Structure
Pyridines / chemical synthesis*
Pyridines / pharmacology*
Solubility
Structure-Activity Relationship
Vascular Endothelial Growth Factor Receptor-2 / antagonists & inhibitors*

Substances

Enzyme Inhibitors
Pyridines
Vascular Endothelial Growth Factor Receptor-2