8-Anilinoimidazo[4,5-g]quinoline-7-carbonitriles as Src kinase inhibitors.
A series of 8-anilinoimidazo[4,5-g]quinoline-7-carbonitriles was synthesized and evaluated as Src kinase inhibitors. Several aniline substituents were surveyed, as well as water-solubilizing groups at the C-2 and N-3 positions. Potent Src inhibitors were identified, with N-3 providing the best position for an additional water-solubilizing group.
Berger
Dan
D
Chemical Sciences, Wyeth-Ayerst Research, Pearl River, NY 10965, USA. bergerd@wyeth.com
Dutia
Minu
M
Powell
Dennis
D
Wu
Biqi
B
Wissner
Allan
A
DeMorin
Frenel
F
Weber
Jennifer
J
Boschelli
Frank
F
D055598:Chemical Phenomena; D002627:Chemistry, Physical; D004791:Enzyme Inhibitors / Q000138:chemical synthesis* / Q000494:pharmacology*; D007202:Indicators and Reagents; D009570:Nitriles / Q000138:chemical synthesis* / Q000494:pharmacology*; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology*; D012995:Solubility; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D004791:Enzyme Inhibitors; D007202:Indicators and Reagents; D009570:Nitriles; D011804:Quinolines; D019061:src-Family Kinases