The new monomer, 5'-O-methacryloyl-3'-azido-3'-deoxythymidine (MAZT), was synthesized from methacryloyl chloride (MAC) and 3'-azido-3'-deoxythymidine (AZT). Poly(MAZT), poly(MAZT-co-&4) and terpolytMAZT-FUR-MAH) were synthesized by radical polymerizations. The average molecular weights of synthesized polymers were in the range of 8,800 -23,ooO depending on polymers. The in vivo antitumor activities of polymers at &oomgkg were increased in the following order : terpoly(MAZT-FUFt-MAH) > poly(MAZT-co-AA) > poly(MAZT) > AZT > 5-FU. The in vitro anti-HW activities of synthesized polymers were less effective than those of AZT and D4T. But the cytotoxicities of the polymers on the MT-4 cell line were found to be much less toxic than AZT.

A series of novel copolymers, poly(methacryloyl-2-oxy-1,2,3-propanetricarboxylic acid-co-exo-3,6-epoxy-1,2,3,6-tetrahydrophthalic acid) [poly(MTCA-co-ETAc)], poly(methacryloyl-2-oxy-1,2,3-propanetricarboxylic acid-cohydrogenethyl-exo-3,6-epoxy-1,2,3,6-tetrahydrophthalate) [poly(MTCA-co-HEET)], and poly(methacryloyl-2-oxy-1,2,3-propanetricarboxylic acid-co-␣-ethoxy-exo-3,6-epoxy-1,2,3,6-tetrahydrophthaloyl-5-fluorouracil) [poly(MTCA-co-EETFU)], were prepared from corresponding monomers by photopolymerizations at 25°C for 48 h. The polymers were identified by FTIR, 1 H-NMR, and 13 C-NMR spectroscopies. The number-average molecular weights of the fractionated polymers determined by GPC were in the range from 9400 to 14,900 and polydispersity indices were 1.2-1.4. The in vitro IC 50 values of polymers against mouse mammary carcinoma (FM3A), mouse leukemia (P388), and human histiocytic lymphoma (U937) as cancer cell lines and mouse liver cells (AC2F) as a normal cell line were much higher compared to that of 5-fluorouracil (5-FU). The in vivo antitumor activities of monomers and polymers against mice bearing sarcoma 180 tumor cell line were better than those of 5-FU. The inhibition of DNA replication and antiangiogenesis activities of MTCA and copolymers were better compared to those of 5-FU.