1.
Bioorg Med Chem Lett
; 20(9): 2924-7, 2010 May 01.
Article
in English
| MEDLINE
| ID: mdl-20363128
ABSTRACT
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.
Subject(s)
Antineoplastic Agents/chemistry , Protein Kinase Inhibitors/chemistry , Quinolines/chemistry , src-Family Kinases/antagonists & inhibitors , Animals , Antineoplastic Agents/chemical synthesis , Antineoplastic Agents/pharmacology , Humans , Mice , Mice, Nude , Microsomes/metabolism , Protein Kinase Inhibitors/chemical synthesis , Protein Kinase Inhibitors/pharmacology , Quinolines/chemical synthesis , Quinolines/pharmacology , Xenograft Model Antitumor Assays , src-Family Kinases/metabolism
2.
Bioorg Med Chem Lett
; 16(15): 3993-7, 2006 Aug 01.
Article
in English
| MEDLINE
| ID: mdl-16735116
ABSTRACT
New 4-phenylamino-3-quinolinecarbonitriles with a 7-ethynyl group substituted by a pyridine, phenyl or thiophene ring containing basic water solubilizing groups were prepared and evaluated as Src kinase inhibitors. Of these new analogs, potent activity was observed with compounds having a (2,4-dichloro-5-methoxyphenyl)amino group at C-4, a methoxy or ethoxy group at C-6, and a pyridyl group bearing a dimethylamine or N-methylpiperazine on the ethynyl group at C-7.
