| 摘要 |
Inhibition of farnesyl transferase, which is an enzyme involved in ras oncogene expression, is effected by coumpounds of formulas (I) and (II) and their enantiomers, diastereomers, and their pharmaceutically acceptable salts, including prodrugs and solvates thereof wherein: r, s and t are 0 or 1; m = 0, 1, 2; p is 0, 1 or 2; X is selected from the group consisting of oxygen, hydrogen or R1, R2, R3; Y is selected from the group consisting of CHR9, SO2, CO, CO2, O, NR10, SO2NR11 and CONR12; R6, R7, R9, R10, R11, R14, R15, R16, R17, R18, R19, R20, R21, R22, R23, R24, R25, R26, R27 and R28 are selected from the group consisting of hydrogen, lower alkyl or substituted alkyl; R4, R5 are selected from the group consisting of hydrogen, halo, nitro, cyano and U-R13; R12 is selected from the group consisting of hydrogen, lower alkyl, aryl, substituted alkyl or aryl; U is selected from the group consisting of sulfur, oxygen, NR14, CO, SO, SO2, CO2, NR15CO2, NR16CONR17, NR18SO2, NR19SO2NR20, SO2NR21, NR22CO, CONR23, PO2R24 and PO3R25 or U is absent; R1, R2, R3, R8 and R13 are selected from the group consisting of hydrogen, alkyl, substituted alkyl, alkenyl, substituted alkenyl, alkynyl, substituted alkynyl, aralkyl, cycloalkyl, aryl, substituted aryl, heterocyclo, substituted heterocyclo; R, S and T are selected from the group consisting of CH2, CO and CH(CH2)pQ wherein Q is NR26R27 or OR28; and A, B, C and D are carbon, oxygen, sulfur or nitrogen, with the proviso that R13 may be hydrogen except when U is SO, SO2, NR15CO2 or NR18SO2.
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