TY - JOUR
T1 - Novel estradiol based metal complexes of Tc-99m
AU - Neto, Carina
AU - Oliveira, Maria Cristina
AU - Gano, Lurdes
AU - Marques, Fernanda
AU - Thiemann, Thies
AU - Santos, Isabel
N1 - Funding Information:
C. Neto thanks Fundação para a Ciência e Tecnologia (FCT) for a Ph.D. grant ( SFRH/BD/31319/2006 ). The authors thank Dr Joaquim Marçalo and Dr Vânia Sousa for performing mass spectra analysis and elemental analysis, respectively. The authors are grateful to Dr João Abrantes for β measurement in the RBA assays. The QITMS instrument was acquired with the support of the Programa Nacional de Reequipamento Científico (Contract REDE/1503/REM/2005-ITN) of FCT and is part of Rede Nacional de Espectrometria de Massa (RNEM).
PY - 2012/6
Y1 - 2012/6
N2 - 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(κ3-12) 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.
AB - 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(κ3-12) 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.
KW - Breast cancer
KW - Estrogen receptor
KW - Rhenium
KW - SPECT imaging
KW - Technetium
KW - Tricarbonyl complexes
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U2 - 10.1016/j.jinorgbio.2012.03.001
DO - 10.1016/j.jinorgbio.2012.03.001
M3 - Article
C2 - 22469776
AN - SCOPUS:84860528917
SN - 0162-0134
VL - 111
SP - 1
EP - 9
JO - Journal of Inorganic Biochemistry
JF - Journal of Inorganic Biochemistry
ER -