Benzodeazaoxaflavins as Sirtuin Inhibitors with Antiproliferative Properties in Cancer Stem Cells
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- 作者：Dante Rotili ; Domenico Tarantino ; Vincenzo Carafa ; Chantal Paolini ; J枚rg Schemies ; Manfred Jung ; Giorgia Botta ; Salvatore Di Maro ; Ettore Novellino ; Christian Steink眉hler ; Ruggero De Maria ; Paola Gallinari ; Lucia Altucci ; Antonello Mai
- 刊名：Journal of Medicinal Chemistry
- 出版年：2012
- 出版时间：September 27, 2012
- 年：2012
- 卷：55
- 期：18
- 页码：8193-8197
- 全文大小：261K
- 年卷期：v.55,no.18(September 27, 2012)
- ISSN：1520-4804
文摘
Inhibition of sirtuins has recently been proposed as a promising anticancer strategy. Some of the new benzodeazaoxaflavins (2a, 2b, and 2d) here reported as SIRT1/2 inhibitors were endowed with pro-apoptotic properties in human U937 leukemia cells and, most importantly, together with the prototype MC2141 (1) displayed antiproliferative effects in cancer stem cells from patients with colorectal carcinoma and glioblastoma multiforme, known to be highly tumorigenic, resistant to conventional cancer chemotherapy, and responsible, at least in part, for cancer relapse or recurrence.