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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| Dokumentumtípus: | Cikk |
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Pergamon Press
2017
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| Sorozat: | 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 |
| Tartalmi kivonat: | 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. |
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| Terjedelem/Fizikai jellemzők: | 797-802 |
| ISSN: | 0960-894X |