Author/Authors :
F. George Njoroge، نويسنده , , Bancha Vibulbhan، نويسنده , , Carmen S. Alvarez، نويسنده , , W. Robert Bishop، نويسنده , , Joanne Petrin، نويسنده , , Ronald J. Doll، نويسنده , , V. Girijavallabhan، نويسنده , , Ashit K. Ganguly، نويسنده ,
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.