Antitumor Activity of Vinyl Polymer Immobilized 5-Fluorouracils through Organosilicon-Amine Spacer Groups via Urea Bonds

Abstract

Abstract The homopolymerization of vinyl monomer immobilized 5-fluorouracils (5FU) through organosilicon-amine spacer groups via urea bonds (KY-20) and the copolymerization of KY-20 with vinyl monomer were carried out by a radical technique to give the homopolymer [Poly(KY-20)] and copolymer [Poly(KY-20/vinyl monomer)], respectively. The antitumor activities of Poly(KY-20) and Poly(KY-20/vinyl monomer) were tested against p388 lymphocytic leukemia by intraperitoneal (i.p.) transplantation/i.p. or oral (p.o.) administration and against Meth-A fibrosarcoma or MM46 mammary adenocarcinoma in mice by subcutaneous (s.c.) implantation/p.o. administration. These 5FU/ organosilicon-amine hybrid polymer conjugates exhibited significant survival effects against p388 leukemia in mice i.p./i.p. or i.p./p.o. Poly(KY-20/HPMA) also showed stronger growth-inhibitory effects against Meth-A fibrosarcoma and MM46 mammary adenocarcinoma in mice s.c./p.o.