Syntheses and antitumor and anti‐aids activities of polymers containing pyrimidine derivative

Abstract

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.

Syntheses and biological activities of polymers containing methacryloyl‐2‐oxy‐1,2,3‐propanetricarboxylic acid or 5‐fluorouracil

“…1,2 Many attempts have been made to reduce the toxic side effects and to obtain excellent antitumor activities. [3][4][5][6][7][8] Polymers containing 5-fluorouracil (5-FU) have been synthesized to obtain higher antitumor activities. 9 -14 We previously reported on syntheses and biological activities of polymeric antitumor compounds such as 5-FU-containing acryl derivative polymers, 9 -15 tetrahydrophthalic acid derivative polymers (TADPs), 16 -23 and methoxyitaconyl polymers, 24 and poly(diallyl ether-co-maleic anhydride) 25 and poly(glycinyl maleamic acid) derivatives 26,27 for some years now.…”

Syntheses, antitumor activities, and antiangiogenesis of a monomer and its medium molecular weight polymers: Maleimidoethanoyl-5-fluorouracil and its polymers

“…[7][8][9][10][11][12][13][14][15][16] We have reported on the syntheses and biological activities of polymeric antitumor agents for many years. [17][18][19][20][21][22][23][24][25][26][27][28][29][30][31][32] The aim of this work was to synthesize antitumor-and antiangiogenesis-active polymers con-taining 5-FU. We synthesized a new monomer, maleimidoethanoyl-5-fluorouracil (MIEFU), from maleimidoethanoyl chloride (MIEC) and 5-FU.…”

Syntheses, antitumour activities and antiangiogenesis of 1,2,3‐tris(ethoxycarbonyl)‐2‐propyl acrylate and its polymers

“…5 Subsequently, many attempts were made to reduce the toxic side‐effects 6–12. We also have reported the syntheses and biological activities of polymeric antitumour agents such as 5‐fluorouracil (5‐FU) containing acryl derivative polymers,13–18 tetrahydrophthalic acid derivative polymers,19–24 poly(diallyl ether‐ co ‐maleic anhydride),25 poly(glycinyl maleic acid) derivatives,26, 27 and methoxyitaconyl‐5‐fluorouracil,28 and discussed their reduced toxicity and improved antitumour activity.…”