Category: 21900-36-7

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. published their research in Journal of Medicinal Chemistry on August 13 ,2020. The article was titled 《Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting》.Name: 3-(tert-Butyl)benzoyl chloride The article contains the following contents:

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. The results came from multiple reactions, including the reaction of 3-(tert-Butyl)benzoyl chloride(cas: 21900-36-7Name: 3-(tert-Butyl)benzoyl chloride)

3-(tert-Butyl)benzoyl chloride(cas: 21900-36-7) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Name: 3-(tert-Butyl)benzoyl chloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics

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. published their research in Journal of Medicinal Chemistry on August 13 ,2020. The article was titled 《Characterization of Conformationally Constrained Benzanilide Scaffolds for Potent and Selective HDAC8 Targeting》.Name: 3-(tert-Butyl)benzoyl chloride The article contains the following contents:

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. The results came from multiple reactions, including the reaction of 3-(tert-Butyl)benzoyl chloride(cas: 21900-36-7Name: 3-(tert-Butyl)benzoyl chloride)

3-(tert-Butyl)benzoyl chloride(cas: 21900-36-7) belongs to organochlorine compounds. The wide structural variety and divergent chemical properties of organochlorides lead to a broad range of names, applications, and properties. Aliphatic organochlorides are often alkylating agents as chlorine can act as a leaving group, which can result in cellular damage.Name: 3-(tert-Butyl)benzoyl chloride

Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics