SKI-606 and beyond

Published: May 29, 2009
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4-Phenylamino-3-quinolinecarbonitriles have been extensively studied by Wyeth as inhibitors of diverse kinases including EGFR, HER-2, and MEK.1,2 Screening of a library of 4-phenylamino-3-quinolinecarbonitriles with various substituents on the 4-phenylamino group identified 1 as an inhibitor of Src kinase3 (Scheme 1). Optimization of this screening lead led to SKI-606, currently in clinical trials for the treatment of solid tumors.4 Subsequent to the discovery that SKI-606 was a potent Src inhibitor, it was determined that this compound was also a potent inhibitor of Abl kinase.5

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Boschelli, D., Boschelli, F., Wu, B., Ye, F., Wang, Y., Golas, J., Young, T., & Lucas, J. (2009). SKI-606 and beyond. Hematology Meeting Reports (formerly Haematologica Reports), 1(8). https://doi.org/10.4081/hmr.v1i8.278