title: Metal complex SERMs (selective oestrogen receptor modulators). The influence of different metal units on breast cancer cell antiproliferative effects.
abstract: The selective oestrogen receptor modulator tamoxifen is a leading agent in the adjuvant treatment of breast cancer. Several organometallic moieties have been vectorised with tamoxifen, in order to improve on the latter's antiproliferative properties by the addition of a potentially cytotoxic moiety, and have been evaluated versus both oestrogen receptor positive (MCF7) and oestrogen receptor negative (MDA-MB231) breast cancer cells. For tamoxifen analogues with ((R,R)-trans-1,2-diaminocyclohexane)platinum(II), cyclopentadienyl rhenium tricarbonyl, and ruthenocene tethers, there was no enhancement of the antiproliferative effect on oestrogen receptor positive cells, nor any cytotoxic effect on oestrogen receptor negative cells, while those containing cyclopentadienyl titanium dichloride showed an oestrogenic effect. However, compounds where ferrocene replaces tamoxifen's phenyl ring were strongly cytotoxic against both cell lines. The synthesis and biological results of these compounds is reviewed and placed in the historic context of inorganic compounds in therapy.
authors.affiliation: Laboratoire de Chimie et Biochimie des Complexes Molèculaires, UMR CNRS 7576, Ecole Nationale Supèrieure de Chimie de Paris, 11 rue Pierre et Marie Curie, 75231, Paris cedex 05, France.
authors.forename: Anne
authors.initials: A
authors.lastname: Vessières
authors.forename: Siden
authors.initials: S
authors.lastname: Top
authors.forename: Wolfgang
authors.initials: W
authors.lastname: Beck
authors.forename: Elizabeth
authors.initials: E
authors.lastname: Hillard
authors.forename: Gérard
authors.initials: G
authors.lastname: Jaouen
mesh_terms: D000970:Antineoplastic Agents / Q000737:chemistry / Q000633:toxicity*; D001943:Breast Neoplasms / Q000188:drug therapy / Q000473:pathology*; D049109:Cell Proliferation / Q000187:drug effects*; D006801:Humans; D008670:Metals / Q000737:chemistry* / Q000633:toxicity; D020845:Selective Estrogen Receptor Modulators / Q000737:chemistry / Q000633:toxicity*
chemical_list: D000970:Antineoplastic Agents; D008670:Metals; D020845:Selective Estrogen Receptor Modulators