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Cover Picture: Oxidative Metabolism of Ferrocene Analogues of Tamoxifen: Characterization and Antiproliferative Activities of the Metabolites (ChemMedChem 6/2015)
Author(s) -
Richard MarieAude,
Hamels Didier,
Pigeon Pascal,
Top Siden,
Dansette Patrick M.,
Lee Hui Zhi Shirley,
Vessières Anne,
Mansuy Daniel,
Jaouen Gérard
Publication year - 2015
Publication title -
chemmedchem
Language(s) - English
Resource type - Reports
SCImago Journal Rank - 0.817
H-Index - 100
eISSN - 1860-7187
pISSN - 1860-7179
DOI - 10.1002/cmdc.201590015
Subject(s) - hydroxylation , chemistry , cytochrome p450 , tamoxifen , stereochemistry , microsome , biochemistry , metabolism , pharmacology , breast cancer , cancer , in vitro , biology , enzyme , medicine
The front cover picture shows the cytochrome P450‐dependent oxidation of ferrociphenols by rat and human liver microsomes. This oxidation leads to three main classes of metabolites: quinonemethides, indene compounds, and products derived from hydroxylation of the ethyl group. Ferrociphenols are known to exhibit antitumor activity against estrogen‐independent breast cancer cells. Structural identification and synthesis of the major metabolites allowed their evaluation against a human breast cancer cell line, MDA‐MB‐231. A number of the metabolites exhibited remarkable antiproliferative effects toward MDA‐MB‐231 cells. For further details, see the Full Paper by Siden Top, Daniel Mansuy, Gérard Jaouen et al. on p. 981 ff.