| Abstract: | Attachment of anticancer agents to polymers has been demonstrated to improve their therapeutic profiles. A new monomer containing camptothecin, 5‐norbonene‐endo‐2,3‐dicarboxylimidoundecanoyl‐camptothecin (NDUCPT) and its homopolymer and copolymer with acrylic acid (AA) were synthesized and spectroscopically characterized. The NDUCPT content in poly(NDUCPT‐co‐AA) obtained by elemental analysis was 51%. The average molecular weights of the polymers determined by gel permeation chromatography were as follows: Mn = 12 100, Mw = 23 400 g mol?1, Mw/Mn = 1.93 for poly(NDUCPT), Mn = 15 400, Mw = 28 300 g mol?1, Mw/Mn = 1.83 for poly(NDUCPT‐co‐AA). The IC50 value of NDUCPT and its polymers against U937 cancer cells was larger than that of CPT. The in vivo antitumour activity of all polymers in Balb/C mice bearing the sarcoma 180 tumour cell line was greater than that of CPT at a dose of 100 mg kg?1. Copyright © 2003 Society of Chemical Industry |
