Evaluation of novel radioiodinated C7-substituted Δ6,7-estradiol derivatives for molecular recognition of er-positive breast tumours

Carina Neto, Maria Cristina Oliveira, Lurdes Gano, Fernanda Marques, Isabel Santos, Goreti Morais, Takumi Yasuda, Thies Thiemann, Filomena Botelho, Carlos F. Oliveira

Research output: Contribution to journalArticlepeer-review

9 Citations (Scopus)

Abstract

The estrogen receptor is a striking target for molecular imaging and therapy of certain malignancies. In the case of cancer, the ability of imaging the expression of the ER would offer a noninvasive means of classifying tumours guiding the optimal choice of therapy. The importance of estradiol based radioligands as potential imaging agents for estrogen re-ceptor rich tumours and the growing interest in Auger electron emitters for potential radiotherapy of estrogen receptor-positive breast cancers lead to the synthesis and evaluation of a series of radioiodinated derivatives of estradiol. Seeking for new probes for targeting the estrogen receptor two novel radioiodinated Δ6,7-estradiol derivatives containing different C7-alkyl chains were prepared and labelled with 125I. To evaluate the potential use of their 123I-analogues for im-aging breast tumours the biological behaviour of the new radioligands was studied in immature female rats to determine their uptake in and selectivity for tissues containing estrogen receptors. The different alkyl chains induced major modifi-cations in the uptake efficiency, selectivity and in the metabolization degree of the compounds. It is not very clear, how-ever, whether the alterations in uptake efficiency and selectivity are the result of differences in lipophilicity or altered pat-terns of metabolism. Even so, these radioligands exhibit different biological patterns that may be helpful in optimizing the imaging of ER positive tumours.

Original languageEnglish
Pages (from-to)83-91
Number of pages9
JournalCurrent Radiopharmaceuticals
Volume2
Issue number2
DOIs
Publication statusPublished - 2009
Externally publishedYes

Keywords

  • Breast cancer
  • Estradiol
  • Estrogen receptor
  • Radioiodination
  • Spect imaging

ASJC Scopus subject areas

  • Radiology Nuclear Medicine and imaging
  • Pharmacology

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