Farnesyl derivatives and pharmaceutical compositions containing them
AssigneeRamot University Authority for Applied Research and Industrial Development Ltd.
InventorYoel Kloog
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AssigneeRamot University Authority for Applied Research and Industrial Development Ltd.
InventorYoel Kloog
Estimating the term…
Novel farnesyl derivatives which are inhibitors of the prenylated protein thyltransferase enzyme, and useful as anti-cancer drugs, have the following formula: ##STR1## wherein R.sup.1 represents farnesyl, geranyl or geranyl-geranyl; Z represents C--R.sup.6 or N; R.sup.2 represents H, CN, the groups COOR.sup.7, SO.sub.3 R.sup.7, CONR.sup.7 R.sup.8 and SO.sub.2 NR.sup.7 R.sup.7, wherein R.sup.7 and R.sup.8 are each independently hydrogen, alkyl, alkenyl, and the groups COOM and SO.sub.3 M, wherein M is a cation; R.sup.3, R.sup.4, R.sup.5 and R.sup.6 are each independently hydrogen, carboxyl, alkyl, alkenyl, aminoalkyl, nitroalkyl, nitro, halo, amino, mono- or di-alkylamino, mercapto, mercaptoalkyl, azido, or thiocyanato; X represents O, S, SO, SO.sub.2, NH or Se; and the quaternary ammonium salts and N-oxides of the compounds of formula I wherein Z is N.
A compound of the formula:
A pharmaceutical composition comprising a pharmaceutically effective amount of a compound of the formula:
Dependencies are inferred from the claim text.