Tyrphostins. 5. Potent inhibitors of platelet-derived growth factor receptor tyrosine kinase: structure-activity relationships in quinoxalines, quinolines, and indole …

…, H App, G McMahon, J Chen, A Levitzki…

文献索引：Gazit, Aviv; App, Harald; McMahon, Gerald; Chen, Jefferey; Levitzki, Alexander; Bohmer, Frank D. Journal of Medicinal Chemistry, 1996 , vol. 39, # 11 p. 2170 - 2177

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被引用次数: 235

摘要

A series of 3-indoleacrylonitrile tyrphostins, 2-chloro-3-phenylquinolines, and 3- arylquinoxalines were prepared and tested for inhibition of platelet-derived growth factor receptor tyrosine kinase (PDGF-RTK) activity. The potency of the inhibitors was found to be quinoxalines> quinolines> indoles. Lipophilic groups (methyl, methoxy) in the 6 and 7 positions and phenyl at the 3 position of quinoxalines and quinolines were essential for ...