Por favor, use este identificador para citar o enlazar este ítem: https://hdl.handle.net/20.500.12008/52343

Título:

Development and Evaluation of 99mTc Tricarbonyl Complexes Derived from Flutamide with Affinity for Androgen Receptor

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Autor:

Cardoso, María Elena
Decuadra, Paula
Zeni, Maia
Delfino, Agustín
Tejería, Emilia
Coppe, Fátima
Mesa, Juan Manuel
Daher, Grysette
Giglio, Javier
Carrau, Gonzalo
Gamenara, Daniela
Alonso, Omar
Terán, Mariella
Rey, Ana

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Tipo de documento:

Artículo

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Palabras clave:

99mTc
Prostate cancer
Androgen receptor

Descriptores:

DIAGNÓSTICO POR IMAGEN
FLUTAMIDA
FARMACOLOGÍA
COMPUESTOS DE ORGANOTECNECIO
HOMBRES
RADIOFÁRMACOS
RECEPTORES ANDROGÉNICOS
COMPUESTOS DE TECNECIO
NEOPLASIAS DE LA PRÓSTATA

Año de publicación:

2023

Contenido:

Resumen:

With the objective to develop a potential 99mTc radiopharmaceutical for imaging the androgen receptor (AR) in prostate cancer, four ligands bearing the same pharmacophore derived from the ARantagonist flutamide were prepared, labeled with 99mTc, and their structures corroborated via comparison with the corresponding stable rhenium analogs. All complexes were obtained with high radiochemical purity. Three of the complexes were highly stable, and, due to their favorable physicochemical properties, were further evaluated using AR-positive and AR-negative cells in culture. All complexes exhibited considerable uptake in AR-positive cells, which could be blocked by an excess of flutamide. The efflux from the cells was moderate. They also showed significantly lower uptakes in AR-negative cells, indicating interactions with the AR receptor. However, the binding affinities were considerably reduced by the coordination to 99mTc, and the complex that exhibited the best biological behavior did not show sufficient specificity towards AR-positive cells.

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MDPI

EN:

Molecules. 2023;28(2)

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Citación:

Cardoso M, Decuadra P, Zeni M y otros. Development and Evaluation of 99mTc Tricarbonyl Complexes Derived from Flutamide with Affinity for Androgen Receptor. Molecules [en línea]. 2023;28(2). 18 p.

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ISSN:

1420-3049

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Licencia:

Licencia Creative Commons Atribución (CC - By 4.0)

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Publicaciones Académicas y Científicas
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