Synthesis and biological evaluation of 4-phenoxy-phenyl isoxazoles as novel acetyl-CoA carboxylase inhibitors was written by Wu, Xin;Yu, Yongbo;Huang, Tonghui. And the article was included in Journal of Enzyme Inhibition and Medicinal Chemistry in 2021.Reference of 103-16-2 The following contents are mentioned in the article:
Acetyl-CoA carboxylase (ACC) is a crucial enzyme in fatty acid metabolism, which plays a major role in the occurrence and development of certain tumors. Herein, one potential ACC inhibitor () was identified through high-throughput virtual screening (HTVS), and a series of 4-phenoxy-Ph isoxazoles were synthesized for structure-activity relationship (SAR) studies. Among these compounds, exhibited the most potent ACC inhibitory activity (IC50=99.8 nM), which was comparable to that of CP-640186. Moreover, the antiproliferation assay revealed that compound exhibited the strongest cytotoxicity, with IC50 values of 0.22μM (A549), 0.26μM (HepG2), and 0.21μM (MDA-MB-231), resp. The preliminary mechanistic studies on and suggested that the compounds decreased the malonyl-CoA levels, arrested the cell cycle at the G0/G1 phase, and induced apoptosis in MDA-MB-231 cells. Overall, these results indicated that the 4-phenoxy-Ph isoxazoles are potential for further study in cancer therapeutics as ACC inhibitors. This study involved multiple reactions and reactants, such as 4-Benzyloxyphenol (cas: 103-16-2Reference of 103-16-2).
4-Benzyloxyphenol (cas: 103-16-2) belongs to ethers. Esters perform as high-grade solvents for a broad array of plastics, plasticizers, resins, and lacquers, and are one of the largest classes of synthetic lubricants on the commercial market. Polyesters are important plastics, with monomers linked by ester moieties. Esters contain a carbonyl center, which gives rise to 120° C–C–O and O–C–O angles. Unlike amides, esters are structurally flexible functional groups because rotation about the C–O–C bonds has a low barrier. Their flexibility and low polarity is manifested in their physical properties; they tend to be less rigid (lower melting point) and more volatile (lower boiling point) than the corresponding amides. Reference of 103-16-2
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem