摘要 |
PURPOSE: C10 ester substituted taxane is provided which characteristically shows improved antitumor activity. CONSTITUTION: C10 ester substituted taxane is represented by the formula 1, wherein R2 is acyloxy; R7 is hydroxy; R9 is keto, hydroxy or acyloxy; R10 is R10aCOO- wherein R10a is hydrocarbyl, substituted hydrocarbyl, or heterocyclo, provided that hydrocarbyl or substituted hydrocarbyl contains carbon atom at alpha and beta site of R10a substituted carbon; R14 is hydrido or hydroxy; X3 is heterocyclo, or substituted or unsubstituted alkyl, alkenyl or alkynyl wherein alkyl contains 2 or more carbons; X5 is -COX10, -COOX10 or -CONHX10; X10 is hydrocarbyl, substituted hydrocarbyl or heterocyclo; and Ac is acetyl.
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