Identification of selenocompounds with promising properties to reverse cancer multidrug resistance.

Domínguez-Álvarez, Enrique and Gajdács, Márió and Spengler, Gabriella and Palop, Juan Antonio and Marć, Małgorzata Anna and Kieć-Kononowicz, Katarzyna and Amaral, Leonard and Molnár, Joseph and Jacob, Claus and Handzlik, Jadwiga and Sanmartín, Carmen (2016) Identification of selenocompounds with promising properties to reverse cancer multidrug resistance. Bioorganic & medicinal chemistry letters, 26 (12). pp. 2821-4. ISSN 1464-3405

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Abstract

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.

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