Journal
BIOORGANIC CHEMISTRY
Volume 33, Issue 1, Pages 1-15Publisher
ACADEMIC PRESS INC ELSEVIER SCIENCE
DOI: 10.1016/j.bioorg.2004.06.009
Keywords
antitumor agents; breast cancer; estrachol; platinum(II) complexes; hybrid estradiol-Pt(II) complexes
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The synthesis of two new highly potent 17beta-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. (C) 2004 Elsevier Inc. All rights reserved.
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