Marson, Charles M.; Matthews, Christopher J.; Yiannaki, Elena; Atkinson, Stephen J.; Soden, Peter E.; Shukla, Lena; Lamadema, Nermina; Thomas, N. Shaun B. published the artcile< Discovery of Potent, Isoform-Selective Inhibitors of Histone Deacetylase Containing Chiral Heterocyclic Capping Groups and a N-(2-Aminophenyl)benzamide Binding Unit>, Product Details of C10H11NS2, the main research area is aminophenylbenzamide pyrimidine imidazolinone thiazoline capped preparation histone deacetylase inhibition; thiazoline capped HDAC3 NCoR1 inhibitor preparation antitumor activity apoptosis.
The synthesis of a novel series of potent chiral inhibitors of histone deacetylase (HDAC) is described that contain a heterocyclic capping group and a N-(2-aminophenyl)benzamide unit that binds in the active site. In vitro assays for the inhibition of HDAC1, HDAC2, HDAC3-NCoR1, and HDAC8 by the N-(2-aminophenyl)benzamide I gave resp. IC50 values of 930, 85, 12, and 4100 nM, exhibiting class I selectivity and potent inhibition of HDAC3-NCoR1. Both imidazolinone and thiazoline rings are shown to be effective replacements for the pyrimidine ring present in many other 2-(aminophenyl)benzamides previously reported, an example of each ring system at 1 μM causing an increase in histone H3K9 acetylation in the human cell lines Jurkat and HeLa and an increase in cell death consistent with induction of apoptosis. Inhibition of the growth of MCF-7, A549, DU145, and HCT116 cell lines by I was observed, with resp. IC50 values of 5.4, 5.8, 6.4, and 2.2 mM.
Journal of Medicinal Chemistry published new progress about Antitumor agents. 171877-39-7 belongs to class thiazole, and the molecular formula is C10H11NS2, Product Details of C10H11NS2.
Referemce:
Thiazole | C3H3NS – PubChem,
Thiazole | chemical compound | Britannica