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Synthesis and biological activity of medium molecular weight polymers of camptothecin |
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| Authors: | Neung-Ju Lee Sung-Suk Ju Seon-Hee Kim Thomas Brady |
| Institution: | a Department of Premedical Sciences, College of Medicine, Kosin University, Pusan 602-703, South Korea b Department of Polymer Science and Engineering, Pusan National University, Pusan 609-735, South Korea c Department of Biochemistry, College of Medicine, Pusan National University, Pusan 609-735, South Korea d Department of Chemistry, Pusan National University, Pusan 609-735, South Korea e Department of Chemistry and Biochemistry, University of California, San Diego, 9500 Gilman Drive, La Jolla, CA 92093-0358, USA |
| Abstract: | A new monomer, 3,6-endo-methylene-1,2,3,6-tetrahydrophthalimidohexanoylcamptothecin (ETHCPT) was synthesized from 3,6-endo-methylene-1,2,3,6-tetrahydrophthalimidohexanoic acid. Its homopolymer and copolymer with acrylic acid (AA) were synthesized and spectroscopically characterized. The ETHCPT content in poly(ETHCPT-co-AA) obtained by elemental analysis was 37 wt.%. The number-average molecular weights of the polymers determined by gel permeation chromatography were as follows: Mn=9700 for poly(ETHCPT),  for poly(ETHCPT-co-AA). The IC50 value of ETHCPT and its polymers against cancer cells was much larger than that of CPT. The in vivo antitumor activity of all polymers in Balb/C mice bearing the sarcoma 180 tumor cell line was greater than that of CPT at a dose of 100 mg/kg. |
| Keywords: | 3 6-Endo-methylene-1 2 3 6-tetrahydrophthalimidohaxanoylcamptothecin Camptothecin Poly(ETHCPT-co-AA) Photopolymerization In vitro cytotoxicity In vivo antitumor activity |
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