Design and synthesis of small molecule agonists of EphA2 receptor was written by Petty, Aaron;Idippily, Nethrie;Bobba, Viharika;Geldenhuys, Werner J.;Zhong, Bo;Su, Bin;Wang, Bingcheng. And the article was included in European Journal of Medicinal Chemistry in 2018.Recommanded Product: 6834-42-0 This article mentions the following:
Ligand-independent activation of EphA2 receptor kinase promotes cancer metastasis and invasion. Activating EphA2 receptor tyrosine kinase with small mol. agonist is a novel strategy to treat EphA2 overexpressing cancer. In this study, we performed a lead optimization of a small mol. Doxazosin that was identified as an EphA2 receptor agonist. 33 new analogs were developed and evaluated; a structure-activity relationship was summarized based on the EphA2 activation of these derivatives Two new derivative compounds 24 and 27 showed much improved activity compared to Doxazosin. Compound 24 possesses a bulky amide moiety, and compound 27 has a dimeric structure that is very different to the parental compound Compound 27 with a twelve-carbon linker of the dimer activated the kinase and induced receptor internalization and cell death with the best potency. Another dimer with a six-carbon linker has significantly reduced potency compared to the dimer with a longer linker, suggesting that the length of the linker is critical for the activity of the dimeric agonist. To explore the receptor binding characteristics of the new mols., we applied a docking study to examine how the small mol. binds to the EphA2 receptor. The results reveal that compounds 24 and 27 form more hydrogen bonds to EphA2 than Doxazosin, suggesting that they may have higher binding affinity to the receptor. In the experiment, the researchers used many compounds, for example, 2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0Recommanded Product: 6834-42-0).
2-(3-Methoxyphenyl)acetyl chloride (cas: 6834-42-0) belongs to organic chlorides. Chlorination modifies the physical properties of hydrocarbons in several ways. These compounds are typically denser than water due to the higher atomic weight of chlorine versus hydrogen. Aryl chlorides may be prepared by the Friedel-Crafts halogenation, using chlorine and a Lewis acid catalyst.Recommanded Product: 6834-42-0
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics