SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF COPOLYMERS OF N-GLYCINYL MALEIMIDE WITH METHACRYLIC-ACID AND VINYL-ACETATE

Copolymerizations of N-glycinylmaleimide (GMI) with methacrylic acid ( MA) and vinyl acetate (VAc) were carried out in 2-butanone using lauro ylperoxide as an initiator at 70 degrees C. Synthesized GMI, poly(GMI- co-MA), and poly(GMI-co-VAc) were characterized by IR and H-1-NMR spec troscopies, elemental analysis, and gel permeation chromatography. The in vitro cytotoxicities of poly(GMI-co-MA) and poly(GMI-co-VAc) were evaluated using K-562 human leukemia cells and HeLa cells. From the cy totoxicity data against HeLa cells, the copolymers are less cytotoxic than monomeric GMI at dosage of 0.02, 1.0, and 5.0 mg/mL. Copolymers w ere very effective at any dosage tested. The in vivo antitumor activit ies of poly(GMI-co-MA) and poly(GMI-co-VAc) were also evaluated agains t mice bearing sarcoma 180. Monomeric GMI and its copolymers showed hi gher antitumor activity than 5-fluorouracil (5-FU) at any dosage teste d. (C) 1995 John Wiley and Sons, Inc.