Category: 90389-15-4

《A poised fragment library enables rapid synthetic expansion yielding the first reported inhibitors of PHIP(2), an atypical bromodomain》 was published in Chemical Science in 2016. These research results belong to Cox, Oakley B.; Krojer, Tobias; Collins, Patrick; Monteiro, Octovia; Talon, Romain; Bradley, Anthony; Fedorov, Oleg; Amin, Jahangir; Marsden, Brian D.; Spencer, John; von Delft, Frank; Brennan, Paul E.. Electric Literature of C8H10Cl3N The article mentions the following:

Research into the chem. biol. of bromodomains has been driven by the development of acetyl-lysine mimetics. The ligands are typically anchored by binding to a highly conserved asparagine residue. Atypical bromodomains, for which the asparagine is mutated, have thus far proven elusive targets, including PHIP(2) whose parent protein, PHIP, has been linked to disease progression in diabetes and cancers. The PHIP(2) binding site contains a threonine in place of asparagine, and solution screening have yielded no convincing hits. We have overcome this hurdle by combining the sensitivity of X-ray crystallog., used as the primary fragment screen, with a strategy for rapid follow-up synthesis using a chem.-poised fragment library, which allows hits to be readily modified by parallel chem. both peripherally and in the core. Our approach yielded the first reported hit compounds of PHIP(2) with measurable IC50 values by an AlphaScreen competition assay. The follow-up libraries of four poised fragment hits improved potency into the sub-mM range while showing good ligand efficiency and detailed structural data. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-N-methylmethanamine hydrochloride(cas: 90389-15-4Electric Literature of C8H10Cl3N)

1-(2,6-Dichlorophenyl)-N-methylmethanamine hydrochloride(cas: 90389-15-4) belongs to anime. Nitrous acid converts secondary amines (aliphatic or aromatic) to N-nitroso compounds (nitrosamines): R2NH + HNO2 → R2N―NO. Some nitrosamines are potent cancer-inducing substances, and their possible formation is a serious consideration when nitrites, which are salts of nitrous acid, are present in foods or pharmaceutical preparations. Tertiary amines give rise to nitrosamines more slowly; an alkyl group is eliminated as an aldehyde or ketone, along with nitrous oxide, N2O.Electric Literature of C8H10Cl3N

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

In 1984,Journal of Medicinal Chemistry included an article by Meindl, Wolfgang R.; Von Angerer, Erwin; Schoenenberger, Helmut; Ruckdeschel, Gotthard. Formula: C8H10Cl3N. The article was titled 《Benzylamines: synthesis and evaluation of antimycobacterial properties》. The information in the text is summarized as follows:

The synthesis of benzylamines with various N-alkyl chains and substituents in the aromatic system as well as their evaluation on Mycobacterium tuberculosis H 37 Ra were described. The most active compounds: I.HCl (MIC 10.2 μg/mL), II. HCl (MIC 10.2 μg/mL), and III.HCl (MIC 6.4 μg/mL), also had a marked inhibitory effect on M. marinum and M. lufu. The combination of II with aminosalicylic acid, streptomycin, or dapsone had marked supra-additive effects on M. tuberculosis H 37 Ra. In the experiment, the researchers used many compounds, for example, 1-(2,6-Dichlorophenyl)-N-methylmethanamine hydrochloride(cas: 90389-15-4Formula: C8H10Cl3N)

1-(2,6-Dichlorophenyl)-N-methylmethanamine hydrochloride(cas: 90389-15-4) belongs to anime. Acylation is one of the most important reactions of primary and secondary amines; a hydrogen atom is replaced by an acyl group (a group derived from an acid, such as RCOOH or RSO3H, by removal of ―OH, such as RC(=O)―, RS(O)2―, and so on). Reagents may be acid chlorides (RCOC1, RSO2C1), anhydrides ((RCO)2O), or even esters (RCOOR′); the products are amides of the corresponding acids.Formula: C8H10Cl3N

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