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Journal of Bioactive and Compatible Polymers
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Synthesis of New Poly(N-Vinyl Pyrrolidone-Co-Maleic Acid) Peptide Hormone Conjugates with Anticancer Activity

János Pató

Central Research Institute for Chemistry, POB 17 1525, Budapest, Hungary

Melinda Móra

Central Research Institute for Chemistry, POB 17 1525, Budapest, Hungary

Imre Mezö

Semmulweis University Medical School, Puskin u. 9 1080, Budapest, Hungary

János Seprödi

Semmulweis University Medical School, Puskin u. 9 1080, Budapest, Hungary

István Teplán

Semmulweis University Medical School, Puskin u. 9 1080, Budapest, Hungary

Borbála Vincze

National Institute of Oncology, Ráth Gy. u. 7-9 1122, Budapest, Hungary

Adrienn Kálnay

National Institute of Oncology, Ráth Gy. u. 7-9 1122, Budapest, Hungary

István Pályi

National Institute of Oncology, Ráth Gy. u. 7-9 1122, Budapest, Hungary

Gonadotropin releasing hormone (GnRH) is a decapeptide regulating the gonadotropin release in organisms. Its analogues inhibit breast, endometrium and prostatic tumor cell proliferation in vitro. Some analogues were conjugated via the lysine side chain to poly(N-vinyl pyrrolidone-co-maleic acid) using biodegradable and non-biodegradable oligopeptide spacers. The conjugates were prepared by acylation of oligopeptide nitrophenyl esters with the polymeric precursor, poly(N-vinyl pyrrolidone-co-maleic anhydride), by reacting the GnRH analogues with the polymeric active ester. In vitro tests of these products exhibited increased effects on MCF-7 and MDA MB-231 breast, Ishikawa endometrium and PC3 prostatic human tumor cells compared with the parent decapeptides.

Journal of Bioactive and Compatible Polymers, Vol. 14, No. 4, 304-314 (1999)
DOI: 10.1177/088391159901400402
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