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Metallodrug Conjugates with Steroids and Selective Estrogen Receptor Modulators (SERM)

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An overview of conjugates of coordination complexes and organometallic complexes of Pt, Ru, Fe, Re, lanthanoids and other metals with natural and synthetic estrogens and antiestrogens targeting the nuclear estrogen receptors is provided. These conjugates are used as targeted cytotoxic agents or - if radiolabeled - as imaging probes for the detection of estrogen receptor-rich tissues such as hormone-dependent tumours. They are assessed with respect to their estrogen receptor binding affinities, potential synergistic cytotoxic effects in cancer cells and their specificity for tumour over nonmalignant cells and tissues. The mechanisms of their modes of action are discussed. Pertinent literature is covered up to 2008.

Keywords: Targeted metallodrugs; anticancer drugs; estrogen receptor; selective steroid receptor modulators; steroids

Document Type: Research Article


Affiliations: Organic Chemistry Laboratory, University of Bayreuth, Universitaetsstrasse 30, D-95440 Bayreuth, Germany.

Publication date: June 1, 2009

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  • Current Medicinal Chemistry covers all the latest and outstanding developments in medicinal chemistry and rational drug design. Each issue contains a series of timely in-depth reviews written by leaders in the field covering a range of the current topics in medicinal chemistry. Current Medicinal Chemistry is an essential journal for every medicinal chemist who wishes to be kept informed and up-to-date with the latest and most important developments.

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