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

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 adenocarcinom...

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Bibliographic Details
Main Authors: Gajdács Márió
Spengler Gabriella
Sanmartín Carmen
Marć Małgorzata Anna
Handzlik Jadwiga
Domínguez-Álvarez Enrique
Format: Article
Published: Pergamon Press 2017
Series:BIOORGANIC & MEDICINAL CHEMISTRY LETTERS 27 No. 4
doi:10.1016/j.bmcl.2017.01.033

mtmt:3179770
Online Access:http://publicatio.bibl.u-szeged.hu/10711
Description
Summary: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.
Physical Description:797-802
ISSN:0960-894X