Macromolecular Conjugates of Methotrexate, Ferrocene and Platinum in Cancer Chemotherapy
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Most of the polyaspartamide carrier polymers synthesized in this program, were conjugated with methotrexate (MTX) and with organoiron compound (ferrocene), whereas other polyamides were conjugated with 1,2-diaminocyclohexanediaquaplatinum(II)dinitrate (DACH-Pt aq). The ferrocenylation agent throughout this project was 4-ferrocenylbutanoic acid. MTX and 4-ferrocenylbutanoic acid as well as folic acid were conjugated to pendant amino groups of various polyaspartamide carriers, through amidation reactions, via the HBTU-method. A very satisfactory degree of MTX and Fe were achieved. MTX content found was in range of 10–19% by mass, and Fe content found was in range of 6–13% by mass. The anchoring of platination agent (DACH-Pt aq) proceeded via well established methods involving dihydroxylato ligands. Pt content found was in the range of 6–8% by mass. Platinum incorporation was satisfactory.
KeywordsPolymer Amine Carrier Polyaspartamide Conjugate Anchoring
The authors gratefully acknowledge the bursary supports provided by the Foundation for Research Development, NRF, (2007–2008), Bradlow Postgraduate Awards (2006–2009) of this University and the donation of Platinum salt from Angloplatinum.
- 5.A.I. Mufula, Macromolecular derivatives of Methotrexate and Ferrocene as potential prodrugs in cancer chemotherapy, MSc. Dissertation, School of Chemistry, Wits University (2010)Google Scholar
- 6.A.I. Mufula, E.W. Neuse, Macromolecular Carriers for Methotrexate and Ferrocene in Cancer Chemotherapy. J. Inorg. Organomet. Polym. Mater. (2011). doi: 10.1007/s10904-011-9471-0
- 11.P. Öhrngren, J. Georgsson, Synthesis of a Hepatitis C Virus NS3 Serine Protease Inhibitor with a Novel Peptidomimetic Scaffold, MSc. Dissertation, Department of Medecinal Chemistry, Faculty of Pharmacy, Uppsala University (2004)Google Scholar
- 17.M.G. Meirim, E.W. Neuse, Polymer conjugated anticancer Drugs, M.Sc. dissertation, School of Chemistry, Wits University (2002)Google Scholar
- 18.F.M. Veronese, M. Morpurgo, Il Farmoco 54, 497 (1999)Google Scholar