| 摘要 |
PURPOSE: To obtain a readily synthesized combretastatin derivative useful as a carcinostatic agent having low toxicity and high therapeutic effects. CONSTITUTION: This stilbene derivative of formula I (X is H or nitrile; Y is an L-α-amino acid acyl), e.g. (Z)-1-(3-amino-4-methoxyphenyl)-2(3,4,5- trimethoxyphenyl)-ethene-glycinamide. The derivative of formula I is obtained by reacting (Z)-1-(3-amino-4-methoxyphenyl)2-(3,4,5-trimethoxyphenyl)-ethene of formula II with an N-α-9-fluorenylmethoxycarbonylamino acid derivative of formula III (Fmoc is N-α-9-fluorenylmethoxycarbonyl; AA is an amino acid acyl) in the presence of dicyclohexylcarbodiimide and 1-hydroxybenzotriazole in dimethylformamide at ambient temperature for 6-12hr, purifying the resultant compound and then deprotecting the purified compound with aqueous sodium hydroxide. The compound of formula I as a carcinostatic agent is usually used in a dose of 1-3000mg for an adult and daily 1-9000mg divided into several portions.
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