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

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• 作者：Má ; rió ; Gajdá ; cs^a ; Gabriella Spengler^a ; Carmen Sanmartí ; n^b ; Małgorzata Anna Marć^c ; Jadwiga Handzlik^c ; Enrique Domí ; nguez-Á ; lvarez^b ; ^c ; ^{enriquedominguezalv@gmail.com}
• 关键词：Selenium ; Multidrug resistance (MDR) ; Selenoesters ; Cancer ; Apoptosis ; MDR efflux pumps ; ABCB1 efflux pump (P-glycoprotein)
• 刊名：Bioorganic & Medicinal Chemistry Letters
• 出版年：2017
• 出版时间：15 February 2017
• 年：2017
• 卷：27
• 期：4
• 页码：797-802
• 全文大小：791 K
• 卷排序：27

文摘

Active anticancer selenocompounds were evaluated in colon adenocarcinoma cells. Their selective, cytotoxic, proapoptotic and MDR reversal activity were determined. At 2 μM, 4 compounds reversed MDR more strongly than reference verapamil at 20 μM. In cytotoxicity assay in Colo 320 cells, 3 compounds showed nanomolar IC50 values. 4 compounds triggered apoptotic events in >60% of the gated colon cancer cells.