Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells

Dante Rotili; Domenico Tarantino; Vincenzo Carafa; Chantal Paolini; Jörg Schemies; Manfred Jung; Giorgia Botta; Salvatore Di Maro; Ettore Novellino; Christian Steinkühler; Ruggero De Maria; Paola Gallinari; Lucia Altucci; Antonello Mai

doi:10.1021/jm301115r

Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells

Dante Rotili, Domenico Tarantino, Vincenzo Carafa, Chantal Paolini, Jörg Schemies, Manfred Jung, Giorgia Botta, Salvatore Di Maro, Ettore Novellino, Christian Steinkühler, Ruggero De Maria, Paola Gallinari, Lucia Altucci, Antonello Mai

Istituto Regina Elena

Research output: Contribution to journal › Article › peer-review

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.

Original language	English
Pages (from-to)	8193-8197
Number of pages	5
Journal	Journal of Medicinal Chemistry
Volume	55
Issue number	18
DOIs	https://doi.org/10.1021/jm301115r
Publication status	Published - Sep 27 2012

ASJC Scopus subject areas

Molecular Medicine
Drug Discovery

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Rotili, D., Tarantino, D., Carafa, V., Paolini, C., Schemies, J., Jung, M., Botta, G., Di Maro, S., Novellino, E., Steinkühler, C., De Maria, R., Gallinari, P., Altucci, L., & Mai, A. (2012). Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells. Journal of Medicinal Chemistry, 55(18), 8193-8197. https://doi.org/10.1021/jm301115r

Rotili, D, Tarantino, D, Carafa, V, Paolini, C, Schemies, J, Jung, M, Botta, G, Di Maro, S, Novellino, E, Steinkühler, C, De Maria, R, Gallinari, P, Altucci, L & Mai, A 2012, 'Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells', Journal of Medicinal Chemistry, vol. 55, no. 18, pp. 8193-8197. https://doi.org/10.1021/jm301115r

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AU - Rotili, Dante

AU - Tarantino, Domenico

AU - Carafa, Vincenzo

AU - Paolini, Chantal

AU - Schemies, Jörg

AU - Jung, Manfred

AU - Botta, Giorgia

AU - Di Maro, Salvatore

AU - Novellino, Ettore

AU - Steinkühler, Christian

AU - De Maria, Ruggero

AU - Gallinari, Paola

AU - Altucci, Lucia

AU - Mai, Antonello

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AB - 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.

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Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells

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