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 | |
| Publication status | Published - Sep 27 2012 |
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ASJC Scopus subject areas
- Molecular Medicine
- Drug Discovery
Cite this
Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells. / Rotili, Dante; Tarantino, Domenico; Carafa, Vincenzo; Paolini, Chantal; Schemies, Jörg; Jung, Manfred; Botta, Giorgia; Di Maro, Salvatore; Novellino, Ettore; Steinkühler, Christian; De Maria, Ruggero; Gallinari, Paola; Altucci, Lucia; Mai, Antonello.
In: Journal of Medicinal Chemistry, Vol. 55, No. 18, 27.09.2012, p. 8193-8197.Research output: Contribution to journal › Article
}
TY - JOUR
T1 - Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells
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
PY - 2012/9/27
Y1 - 2012/9/27
N2 - 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.
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.
UR - http://www.scopus.com/inward/record.url?scp=84866849116&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=84866849116&partnerID=8YFLogxK
U2 - 10.1021/jm301115r
DO - 10.1021/jm301115r
M3 - Article
C2 - 22931526
AN - SCOPUS:84866849116
VL - 55
SP - 8193
EP - 8197
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 18
ER -