title: N,N'-Bisbenzylidenebenzene-1,4-diamines and N,N'-Bisbenzylidenenaphthalene-1,4-diamines as Sirtuin Type 2 (SIRT2) Inhibitors.
abstract: A series of N,N'-bisbenzylidenebenzene-1,4-diamine and N,N'-bisbenzylidenenaphthalene-1,4-diamine derivatives were synthesized as inhibitors for human sirtuin type 2 (SIRT2). The design of the new compounds was based on two earlier reported hits from molecular modeling and virtual screening. The most potent compound was N,N'-bis(2-hydroxybenzylidene)benzene-1,4-diamine, which was equipotent with the most potent hit compound and well-known SIRT2 inhibitor sirtinol.
authors.affiliation: Department of Pharmaceutical Chemistry , University of Kuopio, P.O. Box 1627, 70211 Kuopio, Finland. paivi.kiviranta@uku.fi
authors.forename: Päivi H
authors.initials: PH
authors.lastname: Kiviranta
authors.forename: Jukka
authors.initials: J
authors.lastname: Leppänen
authors.forename: Sergiy
authors.initials: S
authors.lastname: Kyrylenko
authors.forename: Heikki S
authors.initials: HS
authors.lastname: Salo
authors.forename: Maija
authors.initials: M
authors.lastname: Lahtela-Kakkonen
authors.forename: Anu J
authors.initials: AJ
authors.lastname: Tervo
authors.forename: Carsten
authors.initials: C
authors.lastname: Wittekindt
authors.forename: Tiina
authors.initials: T
authors.lastname: Suuronen
authors.forename: Erkki
authors.initials: E
authors.lastname: Kuusisto
authors.forename: Tomi
authors.initials: T
authors.lastname: Järvinen
authors.forename: Antero
authors.initials: A
authors.lastname: Salminen
authors.forename: Antti
authors.initials: A
authors.lastname: Poso
authors.forename: Erik A A
authors.initials: EA
authors.lastname: Wallén
mesh_terms: D000107:Acetylation; D001665:Binding Sites; D003959:Diamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D015394:Molecular Structure; D010655:Phenylenediamines / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D056565:Sirtuin 2; D037761:Sirtuins / Q000037:antagonists & inhibitors* / Q000378:metabolism; D013329:Structure-Activity Relationship
chemical_list: D003959:Diamines; C516689:N,N'-bis(2-hydroxybenzylidene)benzene-1,4-diamine; D010655:Phenylenediamines; C474199:SIRT2 protein, human; D056565:Sirtuin 2; D037761:Sirtuins