Detalle Publicación

Identification of selenocompounds with promising properties to reverse cancer multidrug resistance

Autores: Domínguez Álvarez, Enrique; Gajdács, M.; Spengler, G.; Palop Cubillo, Juan Antonio; Marc, M.; (Kiec-Kononowicz, K.; Amaral, L.; Molnár, J.; Jacob, C.; Handzlik, J.; Sanmartín Grijalba, Carmen
Título de la revista: BIOORGANIC AND MEDICINAL CHEMISTRY LETTERS
ISSN: 0960-894X
Volumen: 26
Número: 12
Páginas: 2821 - 2824
Fecha de publicación: 2015
Resumen:
In previous studies, 56 novel selenoesters and one cyclic selenoanhydride with chemopreventive, antiproliferative and cytotoxic activity were described. Herein, the selenoanhydride and selected selenoesters were evaluated for their ability to reverse the cancer multidrug resistance (MDR) using the ABCB1 efflux pump inhibition assay in mouse MDR T-lymphoma cells. Results showed that the selenoanhydride (1) and the selenoesters with ketone terminal fragments (9-11) exerted (1.7-3.6)-fold stronger efflux pump inhibitory action than the reference verapamil. In addition, those four derivatives triggered apoptotic events in more than 80% of the examined MDR mouse cells.
DOI: https://doi.org/10.1016/j.bmcl.2016.04.064
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