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Antitumoral Activity Induced by Alkylating Agents Conjugated to Poly(maleic anhydride-alt-vinyl acetate)

Department of Natural and Synthetic Polymers, "Gh.Asachi" Technical University of Iai, Bd. D. Mangeron, No 71 A, 700050 Iai, Romania, marpopa{at}ch.tuiasi.ro

Valeriu Sunel

Department of Organic Chemistry, "Al.I.Cuza" University of Iai, Bd. Carol No 11, 700506, Iai, Romania

Nicoleta Dulea

Department of Organic Chemistry, "Al.I.Cuza" University of Iai, Bd. Carol No 11, 700506, Iai, Romania

Aura Angelica Popa

"Petre Andrei" University, Str. Ghica Voda, No. 13, 700400, Iasi, Romania

Raphael M. Ottenbrite

Virginia Commonwealth University, Richmond, USA

Constantin V. Uglea

Department of Biomedical Engineering, University of Medicine and Pharmacy, Str. Universitatii 16, 700015 Iasi, Romania

New polyanionic polymer conjugates with antitumoral activity are synthesized by chemically binding mustard type alkylating derivatives of di-(ß-chloroethyl)-amine and tri-(ß-chloroethyl)-amine, respectively, onto poly(maleic anhydride-alt-vinyl acetate). The structures of the compounds are verified by FTIR, ¹H NMR, and elemental analysis. The antitumoral activity of these polymeric drugs is evaluated in vivo using carcinosarcoma Walker 256 solid tumors in Wister rats. The conjugates exhibit antitumor regression (ATR) values between 25 and 44% depending on comonomers' structure. In addition, an accumulation in the solid tumors (enhanced permeability and retention (EPR) effect) by these compounds is observed. These compounds also cause small organotropic effects, such as increases in the liver, spleen, and kidney weight.

Key Words: poly(maleic anhydride-alt-vinyl acetate) • tri-(ß-chloroethyl)-amine • di-(ß-chloroethyl)-amine • antitumoral activity • bioactive polymers • carcinosarcoma Walker 256 • tumors.

Journal of Bioactive and Compatible Polymers, Vol. 22, No. 6, 651-666 (2007)
DOI: 10.1177/0883911507084424


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