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.
authors.affiliation: Istituto Pasteur-Fondazione Cenci Bolognetti, Dipartimento di Chimica e Tecnologie del Farmaco, Sapienza Università di Roma, Piazzale Aldo Moro 5, 00185 Roma, Italy.
authors.forename: Dante
authors.initials: D
authors.lastname: Rotili
authors.forename: Domenico
authors.initials: D
authors.lastname: Tarantino
authors.forename: Vincenzo
authors.initials: V
authors.lastname: Carafa
authors.forename: Chantal
authors.initials: C
authors.lastname: Paolini
authors.forename: Jörg
authors.initials: J
authors.lastname: Schemies
authors.forename: Manfred
authors.initials: M
authors.lastname: Jung
authors.forename: Giorgia
authors.initials: G
authors.lastname: Botta
authors.forename: Salvatore
authors.initials: S
authors.lastname: Di Maro
authors.forename: Ettore
authors.initials: E
authors.lastname: Novellino
authors.forename: Christian
authors.initials: C
authors.lastname: Steinkühler
authors.forename: Ruggero
authors.initials: R
authors.lastname: De Maria
authors.forename: Paola
authors.initials: P
authors.lastname: Gallinari
authors.forename: Lucia
authors.initials: L
authors.lastname: Altucci
authors.forename: Antonello
authors.initials: A
authors.lastname: Mai
mesh_terms: D000970:Antineoplastic Agents / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D017209:Apoptosis / Q000187:drug effects; D002453:Cell Cycle / Q000187:drug effects; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D002470:Cell Survival / Q000187:drug effects; D005415:Flavins / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology*; D056572:Histone Deacetylase Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology; D006801:Humans; D014411:Neoplastic Stem Cells / Q000187:drug effects* / Q000473:pathology*; D037761:Sirtuins / Q000037:antagonists & inhibitors*
chemical_list: D000970:Antineoplastic Agents; D005415:Flavins; D056572:Histone Deacetylase Inhibitors; D037761:Sirtuins