| 摘要 |
The present invention is directed to betulinol derivatives and betulinol-antibody conjugates having the formulae: and <paragraph lvl="0"><in-line-formula>HO-antibody-spacer-(A2)n </in-line-formula>wherein A1 is a moiety having the formula: A2 is a moiety having the formula: n is an integer from 1 to 100; X and Y1 are each independently selected from the group consisting of a hydroxy group, an alkoxy group, an alkanoyloxy group, and a-peptide-NHNH-C(O)-antibody-OH moiety; Y2 is selected from the group consisting of a hydroxy group, an alkoxy group, and an alkanoyloxy group; and HO-antibody-H is an antibody and, in particular, betulinol dimethyl ether. Methods for making and using these derivatives and conjugates, as well as a method for making and using betulonic aldehyde, are also disclosed.
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