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. © 2012 American Chemical Society.
Rotili, D., Tarantino, D., Carafa, V., Paolini, C., Schemies, J., Jung, M., Botta, G., Di Maro, S., Novellino, E., Steinkühler, C., De Maria Marchiano, R., Gallinari, P., Altucci, L., Mai, A., Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells, <<JOURNAL OF MEDICINAL CHEMISTRY>>, 2012; 55 (18): 8193-8197. [doi:10.1021/jm301115r] [http://hdl.handle.net/10807/112163]
Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells
Rotili, Dante;Botta, Giorgia;Novellino, Ettore;De Maria Marchiano, Ruggero;
2012
Abstract
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. © 2012 American Chemical Society.
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