| 摘要 |
Disclosed are 7-substituted taxoid derivatives, in particular taxol-7-carbazates which have improved water-solubility and/or enhanced therapeutic activity and methods of making the same. The preferred taxoid derivatives have the formula: <IMAGE> wherein Z is H or <IMAGE> Y=O or S; X=CH2 or O; n=zero or a positive integer, preferably one; with the proviso that when n=O, X=CH2; R=C1-C4 alkyl, haloalkyl, carboxyalkyl, thioalkyl, sulfonylalkyl, phenyl, hydroxyphenyl, aminophenyl, carboxyphenyl, a polyalkyleneoxide homopolymer or water soluble polyalkyleneoxide containing copolymer, having a molecular weight of from about 1,000 to about 20,000; <IMAGE> W=O, N-L, S or SO2; Ph is a phenyl group; L=H, C1-C4 alkyl or phenyl; and R2=C1-C4 alkyl, phenyl or a polyalkyleneoxide homopolymer or water soluble polyalkyleneoxide containing copolymer, having a molecular weight of from about 1,000 to about 20,000.
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