title: Novel estradiol based metal complexes of Tc-99m.
abstract: Aiming to contribute to the design of technetium imaging agents for estrogen receptor (ER) positive breast tumors, we have synthesized and evaluated the novel organometallic estradiol complexes (fac-[M(CO)(3)(κ(3)-10)](+) and fac-[M(CO)(3)(κ(3)-12) M=Re/(99m)Tc) using two different bifunctional tridentate ligands (4 and 8). The rhenium complexes (13 and 14) were fully characterized by IR, (1)H NMR, (13)C NMR, mass spectrometry and elemental analyses. The (99m)Tc complexes (15 and 16) were obtained with high radiochemical purity and exhibited high in vitro radiochemical stability. To get a first insight into the relevance of these complexes for targeting ER positive tumors, ER binding affinity assays and cellular internalization studies in an ER expressing cell line, MCF-7, have also been performed suggesting a non ER mediated uptake.
authors.affiliation: Unidade de Ciências Químicas e Radiofarmacêuticas, Instituto Tecnológico e Nuclear, Instituto Superior Técnico, Universidade Técnica de Lisboa, Estrada Nacional 10, Sacavém, Portugal.
authors.forename: Carina
authors.initials: C
authors.lastname: Neto
authors.forename: Maria Cristina
authors.initials: MC
authors.lastname: Oliveira
authors.forename: Lurdes
authors.initials: L
authors.lastname: Gano
authors.forename: Fernanda
authors.initials: F
authors.lastname: Marques
authors.forename: Thies
authors.initials: T
authors.lastname: Thiemann
authors.forename: Isabel
authors.initials: I
authors.lastname: Santos
mesh_terms: D001667:Binding, Competitive; D001943:Breast Neoplasms / Q000378:metabolism / Q000473:pathology; D045744:Cell Line, Tumor; D004958:Estradiol / Q000737:chemistry* / Q000378:metabolism; D005260:Female; D006801:Humans; D007700:Kinetics; D009682:Magnetic Resonance Spectroscopy; D013058:Mass Spectrometry; D008956:Models, Chemical; D015394:Molecular Structure; D009942:Organometallic Compounds / Q000138:chemical synthesis / Q000737:chemistry* / Q000378:metabolism; D011960:Receptors, Estrogen / Q000378:metabolism; D012211:Rhenium / Q000737:chemistry* / Q000378:metabolism; D013667:Technetium / Q000737:chemistry* / Q000378:metabolism
chemical_list: D009942:Organometallic Compounds; D011960:Receptors, Estrogen; D004958:Estradiol; D012211:Rhenium; D013667:Technetium