Design and synthesis of 3,7-diarylimidazopyridines as inhibitors of the VEGF-receptor KDR.
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.
Wu
Zhicai
Z
Department of Medicinal Chemistry, Merck Research Laboratories, PO Box 4, West Point, PA 19486, USA. zhicai_wu@merck.com
Fraley
Mark E
ME
Bilodeau
Mark T
MT
Kaufman
Mildred L
ML
Tasber
Edward S
ES
Balitza
Adrienne E
AE
Hartman
George D
GD
Coll
Kathleen E
KE
Rickert
Keith
K
Shipman
Jennifer
J
Shi
Bin
B
Sepp-Lorenzino
Laura
L
Thomas
Kenneth A
KA
D015195:Drug Design; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D011725:Pyridines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012995:Solubility; D013329:Structure-Activity Relationship; D040301:Vascular Endothelial Growth Factor Receptor-2 / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D011725:Pyridines; D040301:Vascular Endothelial Growth Factor Receptor-2