4-Anilino-7-pyridyl-3-quinolinecarbonitriles as Src kinase inhibitors |
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| Authors: | Nan Zhang Biqi Wu Diane H. Boschelli Jennifer M. Golas Frank Boschelli |
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| Affiliation: | 1. Chemical Sciences, Wyeth Research, Pearl River, NY 10965, USA;2. Discovery Oncology, Wyeth Research, Pearl River, NY 10965, USA |
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| Abstract: | A series of 4-anilino-7-pyridyl-3-quinolinecarbonitriles was prepared as Src kinase inhibitors. A systematic SAR study of substitutions on both the pyridine ring and the 3-quinolinecarbonitrile core established the requirements for optimal activity. The lead compound, 17, showed potent activity in both the Src enzyme assay and cell assays, and demonstrated in vivo anti-tumor activity in a xenograft model. |
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