| 摘要 |
<p>A polymer conjugate consisting essentially of: from 90 to 99.9 mol % of units represented by formula (a); from 0.1 to 5 mol % of units represented by formula (b), wherein one of R1 and R2 is a copolymer residue of formula (c), and the other one is hydrogen atom; from 0 to 9.9 mol % of units represented by formula (d), wherein R is a phenyl or t-butoxy group, R3 is H or an acetyl group, A and A1 which may be the same or different, represent a chemical single bond, an amino acid residue or peptide spacer selected from β Ala, Gly, Phe-Gly, Phe-Phe-, Leu-Gly, Val-Ala, Phe-Ala, Leu-Phe, Leu-Ala, Phe-Leu-Gly, Phe-Phe-Leu, Leu-Leu-Gly, Phe-Tyr-Ala, Phe-Gly-Phe, Phe-Phe-Gly, Phe-Leu-Gly-Phe, Gly-Phe-Leu-Gly-Phe, Gly-βAla, Phe-Gly-βAla, Phe-Phe-βAla, Leu-Gly-βAla, Val-Ala-βAla, Phe-Ala-βAla, Leu-Phe-βAla, Leu-Gly-βAla, Phe-Leu-Gly-βAla, Phe-Phe-Leu βAla, Leu-Leu-Gly-βAla, Phe-Tyr-Ala-βAla, Phe-Gly-Phe-β, Phe-Phe-GlyβAla, Phe-Leu-Gly-Phe-βAla or Gly-Phe-Leu-Gly-Phe-βAla. The compounds are endowed with antitumor activity and show improved water solubility and decreased toxicity in comparison with paclitaxel or its known analogs. A method for their preparation and pharmaceutical compositions containing them are also described.</p> |
