Acryloyl‐type polymer fixing 1‐β‐carbonylethyl‐5‐fluorouracil residues through D‐glucofuranoses via ester bonds was synthesized by means of polymerization of the corresponding monomer and polymer reaction. In order to provide the water‐soluble objective polymer, the copolymerization of the acryloyl‐type monomer with acrylamide was carried out. The extent of release of 5‐FU residues from the copolymer was investigated in the enzyme or nonenzyme system in vitro. Furthermore, the antitumor activities of the water‐insoluble homopolymer and water‐soluble copolymer obtained were tested in vivo.
On the course of a series of studies concerned with the elucidation of the allyl polymerization mechanism, the bulk polymerization of allyl benzoate was carried out using a large amount of 2,2′‐azobis(isobutyronitrile) (AIBN) and dimethyl 2,2′‐azobis (isobutyrate) (DMAIB). Incidentally, the initial rate of polymerization initiated by DMAIB was more than two times higher than that by AIBN, although the decomposition rate constants of AIBN and DMAIB are almost same at 80 °C. This peculiar initiation behavior of azo‐initiators is discussed to clarify the initiation mechanism in allyl polymerization, especially focused on the competitive contribution to the initiation and termination reactions by primary radicals.
In order to provide a less toxic 5‐fluorouracil derivative, 1,2:5,6‐di‐O‐isopropylidene‐3‐O‐[3‐(5‐fluorouracill‐yl)‐propionoyl]‐α‐D‐glucofuranose, which was the derivative of 5‐fluorouracil combining indirectly to 3‐position of diacetoneglucose, was synthesized, and its antitumor activity was tested.
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