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 Marchiano; 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 Marchiano, Paola Gallinari, Lucia Altucci, Antonello Mai

Risultato della ricerca: Contributo in rivista › Articolo in rivista

24 Citazioni (Scopus)

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. Â© 2012 American Chemical Society.

Lingua originale	English
pagine (da-a)	8193-8197
Numero di pagine	5
Rivista	Journal of Medicinal Chemistry
Volume	55
DOI	https://doi.org/10.1021/jm301115r
Stato di pubblicazione	Pubblicato - 2012

Keywords

Antineoplastic Agents
Apoptosis
Cell Cycle
Cell Line, Tumor
Cell Proliferation
Cell Survival
Drug Discovery3003 Pharmaceutical Science
Flavins
Histone Deacetylase Inhibitors
Humans
Medicine (all)
Molecular Medicine
Neoplastic Stem Cells
Sirtuins

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10.1021/jm301115r

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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 Marchiano, R., Gallinari, P., Altucci, L., & Mai, A. (2012). Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells. Journal of Medicinal Chemistry, 55, 8193-8197. https://doi.org/10.1021/jm301115r

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title = "Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells",

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. {\^A}{\textcopyright} 2012 American Chemical Society.",

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author = "Dante Rotili and Domenico Tarantino and Vincenzo Carafa and Chantal Paolini and J{\"o}rg Schemies and Manfred Jung and Giorgia Botta and {Di Maro}, Salvatore and Ettore Novellino and Christian Steink{\"u}hler and {De Maria Marchiano}, Ruggero and Paola Gallinari and Lucia Altucci and Antonello Mai",

year = "2012",

doi = "10.1021/jm301115r",

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volume = "55",

pages = "8193--8197",

journal = "Journal of Medicinal Chemistry",

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publisher = "Washington, DC: American Chemical Society",

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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 Marchiano, 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, pagg. 8193-8197. https://doi.org/10.1021/jm301115r

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 Marchiano, Ruggero

AU - Gallinari, Paola

AU - Altucci, Lucia

AU - Mai, Antonello

PY - 2012

Y1 - 2012

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. Â© 2012 American Chemical Society.

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. Â© 2012 American Chemical Society.

KW - Antineoplastic Agents

KW - Apoptosis

KW - Cell Cycle

KW - Cell Line, Tumor

KW - Cell Proliferation

KW - Cell Survival

KW - Drug Discovery3003 Pharmaceutical Science

KW - Flavins

KW - Histone Deacetylase Inhibitors

KW - Humans

KW - Medicine (all)

KW - Molecular Medicine

KW - Neoplastic Stem Cells

KW - Sirtuins

KW - Antineoplastic Agents

KW - Apoptosis

KW - Cell Cycle

KW - Cell Line, Tumor

KW - Cell Proliferation

KW - Cell Survival

KW - Drug Discovery3003 Pharmaceutical Science

KW - Flavins

KW - Histone Deacetylase Inhibitors

KW - Humans

KW - Medicine (all)

KW - Molecular Medicine

KW - Neoplastic Stem Cells

KW - Sirtuins

UR - http://hdl.handle.net/10807/112163

U2 - 10.1021/jm301115r

DO - 10.1021/jm301115r

M3 - Article

SN - 0022-2623

VL - 55

SP - 8193

EP - 8197

JO - Journal of Medicinal Chemistry

JF - Journal of Medicinal Chemistry

ER -

Benzodeazaoxaflavins as sirtuin inhibitors with antiproliferative properties in cancer stem cells

Abstract

Keywords

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