| Literature DB >> 27156771 |
Enrique Domínguez-Álvarez1, Márió Gajdács2, Gabriella Spengler2, Juan Antonio Palop3, Małgorzata Anna Marć4, Katarzyna Kieć-Kononowicz4, Leonard Amaral2, Joseph Molnár2, Claus Jacob5, Jadwiga Handzlik4, Carmen Sanmartín3.
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.Entities:
Keywords: ABCB1 efflux pump (P-glycoprotein); Apoptosis; Cancer; MDR efflux pumps; Multidrug resistance (MDR); Selenium; Selenoesters
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Year: 2016 PMID： 27156771 DOI： 10.1016/j.bmcl.2016.04.064
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN： 0960-894X Impact factor: 2.823