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Synthesis 2010(21): 3631-3636  
DOI: 10.1055/s-0030-1258245
PAPER
© Georg Thieme Verlag Stuttgart ˙ New York

Design, Synthesis, and Testing of Polyamine Vectored Iron Chelators

Raymond J. Bergeron*, Shailendra Singh, Neelam Bharti, Yi Jiang
Department of Medicinal Chemistry, University of Florida, Box 100485 JHMHC, Gainesville, FL, 32610-0485, USA
Fax: +1(352)3928406; e-Mail: rayb@ufl.edu;
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Publication History

Received 7 May 2010
Publication Date:
03 September 2010 (online)

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Abstract

Iron chelators have been shown to control the growth of cancer cells in culture by sequestering exogenous iron in the media. Thus, the ligands prevent cellular access to the metal. However, because transferrin provides iron to tumor cells in animals, chelators have not been effective antitumor agents. Polyamine chelator conjugates in which the polyamine vectored ligands into cells were far more active than the free chelators themselves. However, the free ligands were not released from the vector once in the cell. The current study focuses on the synthesis and preliminary evaluation of a polyamine chelator conjugate capable of releasing the free ligand intracellularly via a nonspecific esterase.

Key words

iron - chelator - conjugate - polyamine vector - intracellular esterase