Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting was written by Hassan, Muhammad Murtaza;Israelian, Johan;Nawar, Nabanita;Ganda, Giovanni;Manaswiyoungkul, Pimyupa;Raouf, Yasir S.;Armstrong, David;Sedighi, Abootaleb;Olaoye, Olasunkanmi O.;Erdogan, Fettah;Cabral, Aaron D.;Angeles, Fabrizio;Altintas, Rabia;de Araujo, Elvin D.;Gunning, Patrick T.. And the article was included in Journal of Medicinal Chemistry in 2020.Category: chlorides-buliding-blocks This article mentions the following:
Histone deacetylases (HDACs) are an attractive therapeutic target for a variety of human diseases. Currently, all four FDA-approved HDAC-targeting drugs are nonselective, pan-HDAC inhibitors, exhibiting adverse side effects at therapeutic doses. Although selective HDAC inhibition has been proposed to mitigate toxicity, the targeted catalytic domains are highly conserved. Herein, a series of rationally designed, conformationally constrained, benzanilide foldamers which selectively bind the catalytic tunnel of HDAC8 is described. The series includes benzanilides, MMH371, MMH409, and MMH410, which exhibit potent in vitro HDAC8 activity (IC50 = 66, 23, and 66 nM, resp.) and up to 410-fold selectivity for HDAC8 over the next targeted HDAC. Exptl. and computational analyses of the benzanilide structure docked with human HDAC8 enzyme showed the adoption of a low-energy L-shaped conformer that favors HDAC8 selectivity. The conformationally constrained HDAC8 inhibitors present an alternative biol. probe for further determining the clin. utility and safety of pharmacol. knockdown of HDAC8 in diseased cells. In the experiment, the researchers used many compounds, for example, 3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6Category: chlorides-buliding-blocks).
3-(Trifluoromethyl)benzene-1-sulfonyl chloride (cas: 777-44-6) belongs to organic chlorides. Organic chlorides can cause corrosion in pipelines, valves and condensers, and cause catalyst poisoning. The hydrocarbon processing industry (HPI) and others are affected by damage caused by these substances. Organochlorine compounds are lipophylic, meaning they are more soluble in fat than in water. This gives them a high tenancy to accumulate in the food chain (biomagnification).Category: chlorides-buliding-blocks
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics