摘要 |
PURPOSE: C7 ester substituted taxane is provided which characteristically shoes improved antitumor activity. CONSTITUTION: C7 ester substituted taxane is represented by the formula 1, wherein R2 is acyloxy; R7 is R7aCOO- wherein R7a is hydrocarbyl, substituted hydrocarbyl, or heterocyclo, provided that hydrocarbyl or substituted hydrocarbyl contains carbon atom at alpha and beta site of R7a substituted carbon; R9 is keto, hydroxy or acyloxy; R10 is hydroxy; R14 is hydrido or hydroxy; X3 is substituted or unsubstituted alkyl, alkenyl or alkynyl, phenyl or heterocyclo; X5 is -COX10, -COOX10 or -CONHX10 wherein X10 is hydrocarbyl, substituted hydrocarbyl or heterocyclo; and Ac is acetyl.
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