Inhibition of Src kinase activity by 4-anilino-7-thienyl-3-quinolinecarbonitriles.
Based on a screening lead from a yeast-based assay to identify Src family kinase inhibitors, a series of 4-anilino-7-thienyl-3-quinolinecarbonitriles was prepared. When the thiophene ring was substituted with a water-solubilizing group in a 2,5-, 3,5- or 2,4-pattern, potent inhibition of Src kinase activity was observed.
Wyeth Research, Chemical Sciences and Oncology, Pearl River, NY 10965, USA. bosched@war.wyeth.com
Diane H
DH
Boschelli
Daniel Y
DY
Wang
Fei
F
Ye
Ayako
A
Yamashita
Nan
N
Zhang
Dennis
D
Powell
Jennifer
J
Weber
Frank
F
Boschelli
D000814:Aniline Compounds / Q000737:chemistry / Q000494:pharmacology*; D004791:Enzyme Inhibitors / Q000737:chemistry / Q000494:pharmacology*; D020128:Inhibitory Concentration 50; D007536:Isomerism; D009570:Nitriles / Q000737:chemistry / Q000494:pharmacology*; D011804:Quinolines / Q000737:chemistry / Q000494:pharmacology*; D012441:Saccharomyces cerevisiae / Q000187:drug effects / Q000201:enzymology; D012995:Solubility; D013329:Structure-Activity Relationship; D013876:Thiophenes / Q000737:chemistry; D019061:src-Family Kinases / Q000037:antagonists & inhibitors*
D000814:Aniline Compounds; D004791:Enzyme Inhibitors; D009570:Nitriles; D011804:Quinolines; D013876:Thiophenes; D019061:src-Family Kinases