2028-34-4Relevant articles and documents
Aminothiazoles as Potent and Selective Sirt2 Inhibitors: A Structure-Activity Relationship Study
Schiedel, Matthias,Rumpf, Tobias,Karaman, Berin,Lehotzky, Attila,Oláh, Judit,Gerhardt, Stefan,Ovádi, Judit,Sippl, Wolfgang,Einsle, Oliver,Jung, Manfred
, p. 1599 - 1612 (2016/03/05)
Sirtuins are NAD+-dependent protein deacylases that cleave off acetyl but also other acyl groups from the ε-amino group of lysines in histones and other substrate proteins. Dysregulation of human Sirt2 (hSirt2) activity has been associated with the pathogenesis of cancer, inflammation, and neurodegeneration, which makes the modulation of hSirt2 activity a promising strategy for pharmaceutical intervention. The sirtuin rearranging ligands (SirReals) have recently been discovered by us as highly potent and isotype-selective hSirt2 inhibitors. Here, we present a well-defined structure-activity relationship study, which rationalizes the unique features of the SirReals and probes the limits of modifications on this scaffold regarding inhibitor potency. Moreover, we present a crystal structure of hSirt2 in complex with an optimized SirReal derivative that exhibits an improved in vitro activity. Lastly, we show cellular hyperacetylation of the hSirt2 targeted tubulin caused by our improved lead structure.
Reaction of Triazene 1-Oxides: Novel Synthesis of Solid Arenediazonium Chlorides
Mohamed, Shaaban K.,Gomaa, Mohsen A.-M.,Nour El-Din, Ahmed M.
, p. 166 - 167 (2007/10/03)
Treatment of 1,3-diaryltriazene 1-oxides with oxalyl chloride in dry toluene at room temperature gives only solid arenediazonium chlorides; however, treatment with acetyl and benzoyl chlorides does not afford the corresponding diazonium chlorides.
Hydrogen Bonding and Bond Order in Phenylhydrazones: Structures of Diethyl 2-(o-Methylphenylhydrazono)-3-oxopentanedioate (1) and Two Forms of Diethyl 2-(p-Nitrophenylhydrazono)-3-oxopentanedioate
Drew, Michael G. B.,Vickery, Brian,Willey, Gerald R.
, p. 1530 - 1535 (2007/10/02)
Reaction of diethyl 3-oxopentanedioate with subtitued benzenediazonium salts in 1:1 ratio gives rise to diethyl 2-(phenylhydrazono)-3-oxopentanedioates.Their IR and 1H NMR spectra have been discussed in terms of the intramolecular hydrogen bonding between