Investigation of the effect of varying the 4-anilino and 7-alkoxy groups of 3-quinolinecarbonitriles on the inhibition of Src kinase activity

…, D Yaczko, D Powell, JM Golas, J Lucas…

Index: Boschelli, Diane H.; Ye, Fei; Wu, Biqi; Wang, Yanong D.; Barrios Sosa, Ana Carolina; Yaczko, Deanna; Powell, Dennis; Golas, Jennifer M.; Lucas, Judy; Boschelli, Frank Bioorganic and Medicinal Chemistry Letters, 2003 , vol. 13, # 21 p. 3797 - 3800

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Citation Number: 17

Abstract

Several 7-alkoxy-4-anilino-3-quinolinecarbonitriles were synthesized and evaluated for Src kinase inhibitory activity. Optimal inhibition of both Src enzymatic and cellular activity was seen with analogues having a 2, 4-dichloro-5-methoxyaniline group at C-4. Compound 18, which has a 1-methylpiperidinemethoxy group at C-7, showed in vivo activity in a xenograft model.