| 摘要 |
he present invention provides compounds of nitrophenylcarbamate-based prodrugs of enediynes suitable for use for gene-directed enzyme-prodrug therapy. Said compounds are represented by the formulae as seen above, wherein: R2 represents H, OH, OR or O(CH2)nX(CH2)mR R3 represents H, OH or OR, n is from 1 to 5 m is from 1 to 5 X is O, NH, OCO, OCONH, CONH, NHCO or NHCOO R4 represents H, R, NRR, CONHR, OR, NHCO2R, CO2R, SO2R, NO2 or up to four F atoms and R is lower alkyl optionally substituted with from 1-4 groups which may be the same or different selected from hydroxyl, methoxy, amino, dimethylamino or carboxylic acid groups or as further defined in the specification. Enzymatic activation of the compounds provides pharmaceutical compounds which may be used for the treatment of neoplastic disease.
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