SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF POLYMERS CONTAINING PYRIMIDINEOR CARBOXYL GROUP

A new monomer, methoxyitaconyl-5-fluorouracil (MITFU), was synthesized by the reaction of 5-fluorouracil (5-FU) and methoxyitaconyl chloride . The homopolymers of MITFU and exo-3,6-epoxy-1,2,3,6-tetra-hydrophtha lic anhydride and their copolymers with acrylic acid and/or vinyl acet ate were prepared by the photopolymerizations. The synthesized MITFU a nd polymers were identified by Fourier transform infrared and H-1 nucl ear magnetic resonance spectroscopies. The contents of MITFU in poly(M ITFU-co-AA) and poly(MITFU-co-VAc) determined by elemental analysis we re 45 and 72 mol%, respectively. The weight average molecular weights determined by gel permeation chromatography were in the range of 7200 to 16,500. The in vitro cytotoxicities of samples were evaluated with mouse mammary carcinoma (FM3A), mouse leukemia (P388) and human histio cytic lymphoma (U937) as cancer cell lines. The in vivo antitumor acti vities of synthesized polymers against mice bearing the sarcoma 180 tu mor cell line were greater than those of 5-FU at concentrations of 0.8 and 80 mg/kg. (C) 1997 by John Wiley & Sons, Ltd.