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Novel tricyclic aminoacetyl and sulfonamide inhibitors of Ras farnesyl protein transferase |
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| Authors: | FGeorge Njoroge Bancha Vibulbhan Carmen S Alvarez WRobert Bishop Joanne Petrin Ronald J Doll V Girijavallabhan Ashit K Ganguly |
| Institution: | Schering-Plough Research Institute, Departments of Chemistry and Tumor Biology, 2015 Galloping Hill Road, Kenilworth, New Jersey, 07033, USA |
| Abstract: | Novel tricyclic FPT inhibitors with submicromolar FPT activity are described. Greatly enhanced FPT activity is realized with phthaloyl derivatized amino compound 2k, which showed FPT inhibitory activity of IC50 = 0.66 μM. Sulfonamides 5g and 50 were also found to be potent FPT inhibitor. SAR resulting from a variety of tricyclic amino acids and sulfonamide derivatives is discussed. |
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