title: Synthesis, characterization and binding affinities of rhenium(I) thiosemicarbazone complexes for the estrogen receptor (α/β).
abstract: The binding affinities towards estrogen receptors (ERs) α and β of a set of thiosemicarbazone ligands (HL(n)) and their rhenium(I) carbonyl complexes [ReX(HL(n))(CO)3] (X=Cl, Br) were determined by a competitive standard radiometric assay with [(3)H]-estradiol. The ability of the coordinated thiosemicarbazone ligands to undergo deprotonation and the lability of the ReX bond were used as a synthetic strategy to obtain [Re(hpy)(L(n))(CO)3] (hpy=3- or 4-hydroxypyridine). The inclusion of the additional hpy ligand endows the new thiosemicarbazonate complexes with an improved affinity towards the estrogen receptors and, consequently, the values of the inhibition constant (Ki) could be determined for some of them. In general, the values of Ki for both ER subtypes suggest an appreciable selectivity towards ERα.
authors: Departamento de Química Inorgánica, Universidade de Vigo, E-36310 Vigo, Galicia, Spain.
authors: Ara
authors: A
authors: Núñez-Montenegro
authors: Departamento de Química Inorgánica, Universidade de Vigo, E-36310 Vigo, Galicia, Spain.
authors: Rosa
authors: R
authors: Carballo
authors: Departamento de Química Inorgánica, Universidade de Vigo, E-36310 Vigo, Galicia, Spain. Electronic address: ezequiel@uvigo.es.
authors: Ezequiel M
authors: EM
authors: Vázquez-López
mesh_terms: D047628:Estrogen Receptor alpha / Q000378:metabolism*; D047629:Estrogen Receptor beta / Q000378:metabolism*; D011485:Protein Binding; D012211:Rhenium / Q000737:chemistry*; D013882:Thiosemicarbazones / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism
chemical_list: D047628:Estrogen Receptor alpha; D047629:Estrogen Receptor beta; D013882:Thiosemicarbazones; D012211:Rhenium
keywords: Estrogen receptor; Rhenium complexes; Thiosemicarbazone ligands; Tricarbonyl complexes; X-ray structure