Chloride substituents modify the physical properties of organic compounds in several ways. 3900-89-8, formula is C6H6BClO2, Name is (2-Chlorophenyl)boronic acid. They are typically denser than water due to the presence of chlorine, which has a high atomic weight. Recommanded Product: (2-Chlorophenyl)boronic acid.
Tang, Kai;Zhao, Min;Wu, Ya-Hong;Wu, Qiong;Wang, Shu;Dong, Yu;Yu, Bin;Song, Yihui;Liu, Hong-Min research published 《 Structure-based design, synthesis and biological evaluation of aminopyrazines as highly potent, selective, and cellularly active allosteric SHP2 inhibitors》, the research content is summarized as follows. Src homol.-2-containing protein tyrosine phosphatase 2 (SHP2) encoded by the proto-oncogene PTPN11 is the first identified non-receptor protein tyrosine phosphatase. SHP2 dysregulation contributes to the pathogenesis of different cancers, making SHP2 a promising therapeutic target for cancer therapy. In this article, authors report the structure-guided design based on the well-characterized SHP2 inhibitor SHP099, extensive structure-activity relationship studies (SARs) of aminopyrazines, biochem. characterization and cellular potency. These medicinal chem. efforts lead to the discovery of the lead compound TK-453 I, which potently inhibits SHP2 (SHP2WT IC50 = 0.023μM, ΔTm = 7.01°C) in a reversible and noncompetitive manner. Compound I exhibits high selectivity over SHP2PTP, SHP1 and PTP1B, and may bind at the “tunnel” allosteric site of SHP2 as SHP099. As the key pharmacophore, the aminopyrazine scaffold not only reorganizes the cationic-π stacking interaction with R111 via the novel hydrogen bond interaction between the S atom of thioether linker and T219, but also mediates a hydrogen bond with E250. In vitro studies indicate that I inhibits proliferation of HeLa, KYSE-70 and THP-1 cells moderately and induces apoptosis of Hela cells. Further mechanistic studies suggest that I can decrease the phosphorylation levels of AKT and Erk1/2 in HeLa and KYSE-70 cells.
Recommanded Product: (2-Chlorophenyl)boronic acid, 2-Chlorophenylboronic acid is a useful research compound. Its molecular formula is C6H6BClO2 and its molecular weight is 156.38 g/mol. The purity is usually 95%.
2-Chlorophenylboronic acid used in the preparation of imidazo[1,2-a]pyridine amides which has tuberculostatic activity.
2-Chlorophenylboronic acid is a diphenyl ether that can be used as a building block for the synthesis of benzodiazepine receptor ligands. It has been shown to be an efficient nucleophile, leading to the formation of carbonyl groups in the presence of halides. 2-Chlorophenylboronic acid has also been shown to inhibit p38 kinase activity and may be useful for anticancer therapy., 3900-89-8.
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics