Optimization of 7-alkene-3-quinolinecarbonitriles as Src kinase inhibitors.
The 7-alkene-3-quinolinecarbonitrile 20, a potent inhibitor of Src enzymatic and cellular activity with IC(50) values of 2.1 and 58 nM, respectively, had comparable efficacy to bosutinib in a colon tumor xenograft study.
Boschelli
Diane H
DH
Wyeth Research, Chemical Sciences 401 N. Middletown Road, Pearl River, NY 10965, United States. bosched@wyeth.com
Wang
Daniel
D
Wang
Yan
Y
Wu
Biqi
B
Honores
Erick E
EE
Barrios Sosa
Ana Carolina
AC
Chaudhary
Inder
I
Golas
Jennifer
J
Lucas
Judy
J
Boschelli
Frank
F
D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D006801:Humans; D051379:Mice; D008819:Mice, Nude; D008861:Microsomes / Q000378:metabolism; D047428:Protein Kinase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D011804:Quinolines / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays; D019061:src-Family Kinases / Q000037:antagonists & inhibitors* / Q000378:metabolism
D000970:Antineoplastic Agents; D047428:Protein Kinase Inhibitors; D011804:Quinolines; D019061:src-Family Kinases