摘要
为了改善取代喜树碱的溶解性、抗肿瘤活性和毒副作用,设计合成了十二个新的取代喜树碱20-位羟基酯衍生物。初步的体外抗肿瘤实验结果表明,取代喜树碱的酯衍生物与其母体化合物具有相近的细胞毒,这个结果可能和该类酯在溶液中自活化作用有关。而体内抑制肿瘤试验显示这些新酯衍生物的体内抗肿瘤活性弱于拓扑替康。
Twelve 20-hydroxyl ester analogues of camptothecin were prepared and evaluated for their in vitro antitumor activity. Preliminary cytotoxicity showed that they possessed the same cytotoxicity as parent drug. This result may relate to the self-activation of this kind of ester in aqueous solution. In vivo tumor inhibiting tests of compounds 2,3,7and 11 exhibited that they had weaker antitumor activity than topotecan.
出处
《安徽医药》
CAS
2006年第6期405-409,共5页
Anhui Medical and Pharmaceutical Journal
