NOVEL FARNESYL TRANSFERASE INHIBITORS, PREPARATION THEREOF, AND PHARMACEUTICAL COMPOSITIONS CONTAINING SAME.

摘要

Novel farnesyl transferase inhibitors of general formula (I), preparation thereof, and pharmaceutical compositions containing same. In general formula (I), R1 is Y-S-A1- (where Y is a hydrogen atom, an amino acid residue, a fatty acid residue, an alkyl or alkoxycarbonyl radical, or a radical R4-S-, where R4 is a C1-6 alkyl radical optionally substituted by a phenyl radical, or a radical of general formula (II), wherein A1, X1, Y1, R2, R'2, X2, Y2, X, R3, R'3 and R are as defined below, and A1 is a C1-4 alkylene radical optionally 'alpha'-substituted in the >C(X1)(Y1) grouping by an amino, alkylamino, alkanoylamino or alkoxycarbonylamino radical); X1 and Y1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, a >C=O grouping; R2 is a straight or branched C1-4 alkyl radical optionally substituted by a cyclohexyl radical; R'2 is hydrogen or alkyl; X2 and Y2 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, a >C=O grouping; R3 is a C1-4 alkyl radical optionally substituted by hydroxy, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that, when R3 is an alkyl radical substituted by a hydroxy radical, R3 may form a lactone with the 'alpha'-carboxy radical; R'3 is hydrogen or alkyl; X is an oxygen or sulphur atom; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted phenyl radical. These novel products have anticancer properties.