Tamoxifen Derivatives for Delivery of the Antitumoral (DACH)Pt Group: Selective Synthesis by McMurry Coupling, and Biochemical Behaviour (pages 754–761)
Siden Top, El Bachir Kaloun, Anne Vessières, Guy Leclercq, Ioanna Laïos, Michèle Ourevitch, Christine Deuschel, Michael J. McGlinchey and Gérard Jaouen
Article first published online: 28 JUL 2003 | DOI: 10.1002/cbic.200200550
Potentiation of the known cytotoxic effects of the ((R,R)-trans-1,2-diaminocyclohexane)-platinum(II) fragment [(DACH)Pt] was the aim of this study. We coupled the malonato derivative of [(DACH)Pt] to tamoxifen (to give 1), the most widely used antiestrogen in the treatment of hormone-dependent breast cancers, and also to hydroxytamoxifen, its active metabolite (to give 2). The antiproliferative effect observed with these two complexes on two hormone-dependent breast cancer cell lines (MCF7 and MVLN) appears to be essentially antihormonal, since incorporation of the (DACH)Pt fragment into the tamoxifen skeleton did not cause an increase in the cytotoxicity of the complexes.