Ozcan, Sevil published the artcileOxadiazole-isopropylamides as Potent and Noncovalent Proteasome Inhibitors, Recommanded Product: 2-(4-(tert-Butyl)phenoxy)acetic acid, the publication is Journal of Medicinal Chemistry (2013), 56(10), 3783-3805, database is CAplus and MEDLINE.
Screening of the 50 000 ChemBridge compound library led to the identification of the oxadiazole-isopropylamide I (PI-1833) which inhibited chymotrypsin-like (CT-L) activity (IC50 = 0.60 ¦ÌM) with little effects on the other two major proteasome proteolytic activities, trypsin-like (T-L) and postglutamyl-peptide-hydrolysis-like (PGPH-L). LC-MS/MS and dialysis show that I is a noncovalent and rapidly reversible CT-L inhibitor. Focused library synthesis provided II (PI-1840) with CT-L activity (IC50 = 27 nM). Detailed SAR studies indicate that the amide moiety and the two Ph rings are sensitive toward modifications. Hydrophobic residues, such as Pr or Bu in the para position (not ortho or meta) of the A-ring and a m-pyridyl group as B-ring, significantly improve activity. Compound II (IC50 = 0.37 ¦ÌM) is more potent than I (IC50 = 3.5 ¦ÌM) at inhibiting CT-L activity in intact MDA-MB-468 human breast cancer cells and inhibiting their survival. The activity of II warrants further preclin. investigation of this class as noncovalent proteasome inhibitors.
Journal of Medicinal Chemistry published new progress about 1798-04-5. 1798-04-5 belongs to catalysis-chemistry, auxiliary class Carboxylic acid,Benzene,Ether, name is 2-(4-(tert-Butyl)phenoxy)acetic acid, and the molecular formula is C12H16O3, Recommanded Product: 2-(4-(tert-Butyl)phenoxy)acetic acid.
Referemce:
https://courses.lumenlearning.com/boundless-chemistry/chapter/catalysis/,
Catalysis – Wikipedia