申请人:TANABE SEIYAKU CO., LTD.
公开号:EP0757049A1
公开(公告)日:1997-02-05
A camptothecin derivative comprising a compound of the formula [I]:
wherein R1 is a substituted or unsubstituted lower alkyl group, X1 is a group of the formula: -NHR2 (R2 is a hydrogen atom or a lower alkyl group) or a group of -OH, and Alk is a straight chain or branched chain alkylene group having optionally an oxygen atom in the chain thereof, bound to a polysaccharide having carboxyl groups via an amino acid or a peptide, or a pharmaceutically acceptable salt thereof. Said camptothecin derivatives show enhanced antitumor activities but few side effects unlike conventional anticancer agents, and hence, these compounds are extremely useful as a medicament.
一种喜树碱衍生物,由式[I]化合物组成:
其中 R1 是取代或未取代的低级烷基,X1 是式中的基团:-NHR2(R2为氢原子或低级烷基)或-OH基团,Alk为直链或支链亚烷基,其链中可选择有一个氧原子,通过氨基酸或肽与具有羧基的多糖结合,或其药学上可接受的盐。与传统抗癌剂不同,上述喜树碱衍生物显示出更强的抗肿瘤活性,但副作用很小,因此,这些化合物作为药物非常有用。