4.5 Article

Identification of selenocompounds with promising properties to reverse cancer multidrug resistance

Journal

BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 26, Issue 12, Pages 2821-2824

Publisher

PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2016.04.064

Keywords

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

Funding

  1. Szeged Foundation for Cancer Research
  2. State of Hungary
  3. European Social Fund 'National Excellence Program' [TAMOP 4.2.4. A/2-11-1-2012-0001]
  4. Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences (Hungary)
  5. European Union

Ask authors/readers for more resources

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. (C) 2016 Elsevier Ltd. All rights reserved.

Authors

I am an author on this paper
Click your name to claim this paper and add it to your profile.

Reviews

Primary Rating

4.5
Not enough ratings

Secondary Ratings

Novelty
-
Significance
-
Scientific rigor
-
Rate this paper

Recommended

No Data Available
No Data Available