Synthesis and antitumour activity of medium molecular weight phthalimide polymers of camptothecin

✍ Scribed by Neung-Ju Lee; Sung-Suk Ju; Won-Jei Cho; Seon-Hee Kim; Kyung-Tae Kang; Thomas Brady; Emmanuel A Theodorakis

• Publisher: John Wiley and Sons
• Year: 2003
• Tongue: English
• Weight: 132 KB
• Volume: 52
• Category: Article
• ISSN: 0959-8103
• DOI: 10.1002/pi.1138

✦ Synopsis

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: M~n~ = 12 100, M~w~ = 23 400 g mol^−1^, M~w~/M~n~ = 1.93 for poly(NDUCPT), M~n~ = 15 400, M~w~ = 28 300 g mol^−1^, M~w~/M~n~ = 1.83 for poly(NDUCPT‐co‐AA). The IC~50~ 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