Gc. Kim et al., SYNTHESIS AND BIOLOGICAL-ACTIVITIES OF ENDO-3,6-EPOXY-1,2,3,6-TETRAHYDROPHTHALIMIDE AND ITS POLYMERS, Journal of applied polymer science, 64(13), 1997, pp. 2605-2612
Photocopolymerizations of endo-3,6-epoxy-1,2,3,6-tetrahydrophthalimide
(ETPI) with acrylic acid (AA), vinyl acetate (VAc), and maleic anhydr
ide (MAH) were carried out in a mixed solvent of 2-butanone and aceton
e using 2,2-dimethoxy-2-phenylacetophenone as an initiator at 25 degre
es C. Synthesized ETPI, poly(ETPI), poly(ETPI-co-AA), poly(ETPI-co-VAc
), and poly(ETPI-co-MAH) were characterized by IR and H-1-NMR spectros
copies, elemental analysis, and gel permeation chromatography. The syn
thesized polymers have a number-average molecular weight ((M) over bar
(n)) in the range of 3500-27,400. The in vitro cytotoxicities of poly(
ETPI), poly(ETPI-co-AA), poly(ETPI-co-VAc), and poly(ETPI-co-MAH) agai
nst fibroblast and K-562 human leukemia cells were lower than that of
monomeric ETPI at a low concentration (0.02 mg/mL). The in vivo antitu
mor activities of the polymers were evaluated by the survival time wit
h sarcoma 180 tumor-bearing mice. The polymers showed higher antitumor
activity and lower toxicity than both monomeric ETPI and 5-fluorourac
il at all doses tested. (C) 1997 John Wiley & Sons, Inc.