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

Research output: Contribution to journalArticle

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 languageEnglish
Pages (from-to)8193-8197
Number of pages5
JournalJournal of Medicinal Chemistry
Volume55
Issue number18
DOIs
Publication statusPublished - 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