Design, Synthesis, and Testing of Polyamine Vectored Iron Chelators.

Design, Synthesis, and Testing of Polyamine Vectored Iron Chelators.
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多胺矢量铁螯合剂的设计、合成和测试。

DOI:
10.1055/s-0030-1258245
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发表时间:
2010
期刊:
Synthesis
影响因子:
--
通讯作者:
Jiang,Yi
Jiang,Yi
中科院分区:
--
文献类型:
--
作者:
Bergeron,RaymondJ;Singh,Shailendra;Bharti,Neelam;Jiang,Yi

文献摘要

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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.