Synthesis of 17β-estradiol-linked platinum(II) complexes and their cytocidal activity on estrogen-dependent and -independent breast tumor cells

The synthesis of two new highly potent 17β-estradiol-linked platinum(II) complexes is described. The new molecules are linked at position 16 of the steroid nucleus with an alkyl chain. They are made from estrone in nine chemical steps with an overall yield exceeding 10%. The biological activity of t...

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Bibliographic Details
Published in:Bioorganic chemistry 2005-02, Vol.33 (1), p.1-15
Main Authors: Perron, Valérie, Rabouin, Daniel, Asselin, Éric, Parent, Sophie, C.-Gaudreault, René, Bérubé, Gervais
Format: Article
Language:English
Subjects:
Antitumor agents
Breast cancer
Estradiol
Hybrid estradiol-Pt(II) complexes
Platinum(II) complexes
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Summary:The synthesis of two new highly potent 17β-estradiol-linked platinum(II) complexes is described. The new molecules are linked at position 16 of the steroid nucleus with an alkyl chain. They are made from estrone in nine chemical steps with an overall yield exceeding 10%. The biological activity of these compounds was evaluated in vitro on estrogen dependent and independent (ER + and ER −) human breast tumor cell lines: MCF-7 and MDA-MB-231. The novel compounds prove to be highly cytotoxic against breast cancer cell lines. The most cytotoxic derivative shows high affinity for the estrogen receptor alpha.
ISSN:0045-2068
1090-2120
DOI:10.1016/j.bioorg.2004.06.009