Chlorinated organic compounds are found in nearly every class of biomolecules. 3900-89-8, formula is C6H6BClO2, Name is (2-Chlorophenyl)boronic acid. Alkyl chlorides, as versatile building blocks in organic chemistry, are used in the preparation of alcohols, thioethers, alkenes, alkynes, esters, and Grignard reagents. COA of Formula: C6H6BClO2.
He, Zhangxu;Jiao, Haomiao;An, Qi;Zhang, Xin;Dan, Zengyangzong;Xu, Jiale;Liu, Hongmin;Ma, Liying;Zhao, Wen research published 《 Discovery of novel 4-phenylquinazoline-based BRD4 inhibitors for cardiac fibrosis》, the research content is summarized as follows. Bromodomain containing protein 4 (BRD4), as an epigenetic reader, can specifically bind to the acetyl lysine residues of histones and has emerged as an attractive therapeutic target for various diseases, including cancer, cardiac remodeling and heart failure. Herein, we described the discovery of hit 5 bearing 4-phenylquinazoline skeleton through a high-throughput virtual screen using 2,003,400 compound library (enamine). Then, structure-activity relationship (SAR) study was performed and 47 new 4-phenylquinazoline derivatives toward BRD4 were further designed, synthesized and evaluated, using HTRF assay set up in our laboratory Eventually, we identified compound C-34, which possessed better pharmacokinetic and physicochem. properties as well as lower cytotoxicity against NRCF and NRCM cells, compared to the pos. control JQ1. Using computer-based mol. docking and cellular thermal shift assay, we further verified that C-34 could target BRD4 at mol. and cellular levels. Furthermore, treatment with C-34 effectively alleviated fibroblast activation in vitro and cardiac fibrosis in vivo, which was correlated with the decreased expression of BRD4 downstream target c-MYC as well as the depressed TGF-β1/Smad2/3 signaling pathway. Taken together, our findings indicate that novel BRD4 inhibitor C-34 tethering a 4-phenylquinazoline scaffold can serve as a lead compound for further development to treat fibrotic cardiovascular disease.
3900-89-8, 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., COA of Formula: C6H6BClO2
Referemce:
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics