Selenoesters and selenoanhydrides as novel multidrug resistance reversing agents: A confirmation study in a colon cancer MDR cell line

Márió Gajdács, Gabriella Spengler, Carmen Sanmartín, Małgorzata Anna Marć, Jadwiga Handzlik, Enrique Domínguez-Álvarez

Research output: Contribution to journalArticle

23 Citations (Scopus)

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.

Original languageEnglish
Pages (from-to)797-802
Number of pages6
JournalBioorganic and Medicinal Chemistry Letters
Volume27
Issue number4
DOIs
Publication statusPublished - Jan 1 2017

Keywords

  • ABCB1 efflux pump (P-glycoprotein)
  • Apoptosis
  • Cancer
  • MDR efflux pumps
  • Multidrug resistance (MDR)
  • Selenium
  • Selenoesters

ASJC Scopus subject areas

  • Biochemistry
  • Molecular Medicine
  • Molecular Biology
  • Pharmaceutical Science
  • Drug Discovery
  • Clinical Biochemistry
  • Organic Chemistry

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