title: Targeting the estrogen receptor with metal-carbonyl derivatives of estradiol.
abstract: As part of our program to develop new probes for the estrogen receptor binding domain, we prepared and evaluated a novel 17α-(rhenium tricarbonyl bipyridyl) vinyl estradiol complex. Preparation of the final compound was achieved using the Stille coupling between the preformed brominated rhenium tricarbonyl bipyridine complex and the tributylstannyl vinyl estradiol. Competitive receptor binding assays and stimulatory assays demonstrated that the final complex retained affinity and efficacy comparable to the corresponding pyridyl vinyl estradiol analog, but lower than that of the phenyl vinyl estradiol analog.
authors.affiliation: Department of Chemistry and Chemical Biology, Northeastern University, Boston, MA 02115-5000, USA. r.hanson@neu.edu
authors.forename: Robert N
authors.initials: RN
authors.lastname: Hanson
authors.forename: Rein
authors.initials: R
authors.lastname: Kirss
authors.forename: Emmett
authors.initials: E
authors.lastname: McCaskill
authors.forename: Edward
authors.initials: E
authors.lastname: Hua
authors.forename: Pakamas
authors.initials: P
authors.lastname: Tongcharoensirikul
authors.forename: Sandra L
authors.initials: SL
authors.lastname: Olmsted
authors.forename: David
authors.initials: D
authors.lastname: Labaree
authors.forename: Richard B
authors.initials: RB
authors.lastname: Hochberg
mesh_terms: D001667:Binding, Competitive; D016503:Drug Delivery Systems; D004958:Estradiol / Q000737:chemistry*; D004965:Estrogen Antagonists / Q000737:chemistry / Q000494:pharmacology; D005260:Female; D006801:Humans; D015394:Molecular Structure; D011485:Protein Binding; D011960:Receptors, Estrogen / Q000378:metabolism*; D014753:Vinyl Compounds / Q000737:chemistry* / Q000494:pharmacology
chemical_list: D004965:Estrogen Antagonists; D011960:Receptors, Estrogen; D014753:Vinyl Compounds; D004958:Estradiol