Journal
BIOORGANIC & MEDICINAL CHEMISTRY LETTERS
Volume 27, Issue 4, Pages 797-802Publisher
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmcl.2017.01.033
Keywords
Selenium; Multidrug resistance (MDR); Selenoesters; Cancer; Apoptosis; MDR efflux pumps; ABCB1 efflux pump (P-glycoprotein)
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Funding
- Szeged Foundation for Cancer Research
- European Union
- State of Hungary
- European Social Fund [TAMOP 4.2.4. A/2-11-1-2012-0001]
- Janos Bolyai Research Scholarship of the Hungarian Academy of Sciences
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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. (C) 2017 Elsevier Ltd. All rights reserved.
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