Author/Authors :
F. George Njoroge، نويسنده , , Ronald J. Doll، نويسنده , , Bancha Vibulbhan، نويسنده , , Carmen S. Alvarez، نويسنده , , W. Robert Bishop، نويسنده , , Joanne Petrin، نويسنده , , Paul Kirschmeier، نويسنده , , Nicholas I. Carruthers، نويسنده , , Jesse K. Wong، نويسنده , , Margaret M. Albanese، نويسنده , , John J. Piwinski، نويسنده , , Joseph Catino، نويسنده , , V. Girijavallabhan، نويسنده , , Ashit K. Ganguly، نويسنده ,
Abstract :
A comprehensive structure-activity relationship (SAR) study of novel tricyclic amides has been undertaken. The discovery of compounds that are potent FPT inhibitors in the nanomolar range has been achieved. These compounds are nonpeptidic and do not contain sulfhydryl groups. They selectively inhibit farnesyl protein transferase (FPT) and not geranylgeranyl protein transferase-1 (GGPT-1). They also inhibit H-Ras processing in Cos monkey kidney cells.
