On August 8, 2013, Marson, Charles M.; Matthews, Christopher J.; Yiannaki, Elena; Atkinson, Stephen J.; Soden, Peter E.; Shukla, Lena; Lamadema, Nermina; Thomas, N. Shaun B. published an article.Recommanded Product: H-Phg(4-OH)-OH The title of the article was Discovery of Potent, Isoform-Selective Inhibitors of Histone Deacetylase Containing Chiral Heterocyclic Capping Groups and a N-(2-Aminophenyl)benzamide Binding Unit. And the article contained the following:
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. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Recommanded Product: H-Phg(4-OH)-OH
The Article related to aminophenylbenzamide pyrimidine imidazolinone thiazoline capped preparation histone deacetylase inhibition, thiazoline capped hdac3 ncor1 inhibitor preparation antitumor activity apoptosis and other aspects.Recommanded Product: H-Phg(4-OH)-OH
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