7-(Aryl/heteroaryl-2-ylethynyl)-4-phenylamino-3-quinolinecarbonitr iles as new Src kinase inhibitors: Addition of water solubilizing groups

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- dich...

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Veröffentlicht in:Bioorganic & medicinal chemistry letters 2006-01, Vol.16 (15), p.3993-3997
Hauptverfasser: Wu, Biqi, Sosa, Ana Carolina Barrios, Boschelli, Diane H, Boschelli, Frank, Honores, Erick E, Golas, Jennifer M, Powell, Dennis W, Wang, Yanong D
Format: Artikel
Sprache:eng
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Zusammenfassung: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.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2006.05.015