| Literature DB >> 28126516 |
Márió Gajdács1, Gabriella Spengler1, Carmen Sanmartín2, Małgorzata Anna Marć3, Jadwiga Handzlik3, Enrique Domínguez-Álvarez4.
Abstract
Taking into account that multidrug resistance (MDR) is the main cause for chemotherapeutic failure in cancer treatment and as a continuation of our efforts to overcome this problem we report the evaluation of one cyclic selenoanhydride (1) and ten selenoesters (2-11) in MDR human colon adenocarcinoma Colo 320 cell line. The most potent derivatives (1, 9-11) inhibited the ABCB1 efflux pump much stronger than the reference compound verapamil. Particularly, the best one (9) was 4-fold more potent than verapamil at a 10-fold lower concentration. Furthermore, the evaluated derivatives exerted a potent and selective cytotoxic activity. In addition, they were strong apoptosis inducers as the four derivatives triggered apoptotic events in a 64-72% of the examined MDR Colo 320 human adenocarcinoma cells.Entities:
Keywords: ABCB1 efflux pump (P-glycoprotein); Apoptosis; Cancer; MDR efflux pumps; Multidrug resistance (MDR); Selenium; Selenoesters
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Year: 2017 PMID: 28126516 DOI: 10.1016/j.bmcl.2017.01.033
Source DB: PubMed Journal: Bioorg Med Chem Lett ISSN: 0960-894X Impact factor: 2.823