Novel estradiol based metal complexes of Tc-99m

Carina Neto, Maria Cristina Oliveira, Lurdes Gano, Fernanda Marques, Thies Thiemann, Isabel Santos

Research output: Contribution to journalArticlepeer-review

16 Citations (Scopus)

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)33-10)]+ and fac-[M(CO)33-12) M = Re/99mTc) using two different bifunctional tridentate ligands (4 and 8). The rhenium complexes (13 and 14) were fully characterized by IR, 1H NMR, 13C NMR, mass spectrometry and elemental analyses. The 99mTc 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.

Original languageEnglish
Pages (from-to)1-9
Number of pages9
JournalJournal of Inorganic Biochemistry
Volume111
DOIs
Publication statusPublished - Jun 2012

Keywords

  • Breast cancer
  • Estrogen receptor
  • Rhenium
  • SPECT imaging
  • Technetium
  • Tricarbonyl complexes

ASJC Scopus subject areas

  • Biochemistry
  • Inorganic Chemistry

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