| abstract |
Novel farnesyl transferase inhibitors of general formula (I), <IMAGE> (I) the preparation thereof and pharmaceutical compositions containing said inhibitors, are disclosed. 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 C1-4 alkyl radical optionally substituted by a phenyl radical or a radical of general formula (II) <IMAGE> (II) wherein A1, X, X1, Y1, R'1, R2, R'2 and R are defined as below, and A1 is a C1-4 alkylene radical optionally alpha-substituted in the >C(X1)(Y1) grouping by an amino or alkylamino, dialkylamino, alkanoylamino or alkoxycarbonylamino radical); X1 and Y1 are each a hydrogen atom or, taken together with the carbon atom to which they are attached, form a >C=O grouping; R'1 is hydrogen or a C1-6 alkyl radical; X is an oxygen or sulphur atom; R2 is a C1-6 alkyl, alkenyl or alkynyl radical optionally substituted by hydroxyl, alkoxy, mercapto, alkylthio, alkylsulphinyl or alkylsulphonyl, with the proviso that when R2 is an alkyl radical substituted by a hydroxy radical, R2 can form a lactone with the alpha -carboxy radical; and R'2 is hydrogen or a C1-6 alkyl radical; and R is a hydrogen atom or an optionally substituted alkyl radical or an optionally substituted pheny radical, with the proviso that radical (a) <IMAGE> (a) is in the 3 or 4 position of the naphthyl ring. The novel products have anticancer properties. |