Use of analogues of polyisoprenyl pyrophosphate for inhibiting protein isoprenylation.

摘要

The invention provides the use of a polyisoprenyl pyrophosphate analogue for preparing a pharmaceutical composition suitable for inhibiting protein isoprenylation. The polyisoprenyl pyrophosphate analogue may have formula 1, <CHEM> wherein: Pren represents a C<5><4>-C<7><4> terpenoid group or a derivative thereof; A<1>, A<2>, A<3> and A4 independently represent a direct bond or a C<5>-C<8> alkylene or alkenylene group, optionally substituted; X<1>, X<2>, X<3> and X4 independently represent a direct bond, oxygen, sulphur, imino or methylimino; Y<1>, Y<2> and Y<3> independently represent hydroxy, alkoxy, mercapto, alkylthio, amino, mono- or di-alkylamino, alkyl, alkenyl, alkynyl, cycloalkyl, aryl or arylalkyl, whereby one of Y<1>, Y<2> and Y<3> may also represent a C1/2 -C<7><4> alkyl or alkenyl group; Z<1> and Z<2> independently represent oxygen or sulphur; and n is 0, 1 or 2, preferably 1; or a pharmaceutically acceptable salt thereof. The pharmaceutical composition is suitable for the prophylaxis and/or treatment of carcinomas and for the inhibition of the isoprenylation of a ras protein.