取代喜树碱20S-羟基酯衍生物的合成和抗肿瘤活性  

Synthesis and antitumor activity of 20S-hydroxyl ester derivatives of camptothecin

作　　者：赵亮[1] 潘显道[1] 刘红岩[1] 赵敬华[1] 吕昭云[1] 付昭娣[1] 梁启勇[1] 

机构地区：[1]中国医学科学院中国协和医科大学药物研究所,北京100050

出　　处：《安徽医药》2006年第6期405-409,共5页Anhui Medical and Pharmaceutical Journal

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.

关 键 词：喜树碱 酯衍生物 抗肿瘤活性 3-氨基丙酸 

分 类 号：R914[医药卫生—药物化学] R73-3[医药卫生—药学]