Inhibition of Src kinase activity by 4-anilino-5,10-dihydro-pyrimido[4,5-b]quinolines.
4-(2,4-Dichloro-5-methoxy)anilino-5,10-dihydropyrimido[4,5-b]quinolines are potent inhibitors of Src kinase and Src cellular activity while having no effect on Fyn cellular activity. The corresponding 4-(2,4-dichloro-5-methoxy)anilino-pyrimido[4,5-b]quinolines are much less effective Src inhibitors.
Boschelli
Diane H
DH
Chemical and Screening Sciences, Wyeth Research, 401 N. Middletown Road, Pearl River, NY 10965, USA. bosched@wyeth.com
Powell
Dennis
D
Golas
Jennifer M
JM
Boschelli
Frank
F
D000970:Antineoplastic Agents / Q000138:chemical synthesis; D002455:Cell Division / Q000187:drug effects; D002461:Cell Line, Transformed; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000494:pharmacology; D005347:Fibroblasts / Q000166:cytology; D006801:Humans; D020128:Inhibitory Concentration 50; D011804:Quinolines / Q000138:chemical synthesis* / Q000494:pharmacology; D013329:Structure-Activity Relationship; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D000970:Antineoplastic Agents; D004791:Enzyme Inhibitors; D011804:Quinolines; D019061:src-Family Kinases