He, Zhangxu team published research on Acta Pharmaceutica Sinica B in 2022 | 99769-19-4

Recommanded Product: 3-(Methoxycarbonyl)phenylboronic acid, 3-Methoxycarbonylphenylboronic acid is a useful research compound. Its molecular formula is C8H9BO4 and its molecular weight is 179.97 g/mol. The purity is usually 95%.

3-Methoxycarbonylphenylboronic acid is a reactanct that has been involved in a variety of applications. For instance, it has been used in Suzuki-Miyaura cross-coupling, Iterative cross-coupling of boronate building blocks, cross-coupling with aryl/ alkenyl sulfonates, synthesis of symmetrical biaryls via CuCl catalyzed homocoupling, trifluoromethylation, and cyanation just to name a few of its many uses.

3-Methoxycarbonylphenylboronic acid is a boronate ligand that has been shown to have an interaction with the nitrogen atoms in amines. This compound is used for the Suzuki coupling reaction, which is a chemical reaction between an organoboron compound and an organic electrophile. 3-Methoxycarbonylphenylboronic acid has a helical structure that can be seen by FTIR spectroscopy and it has potent inhibitory activity., 99769-19-4.

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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.

Recommanded Product: 3-(Methoxycarbonyl)phenylboronic acid, 3-Methoxycarbonylphenylboronic acid is a useful research compound. Its molecular formula is C8H9BO4 and its molecular weight is 179.97 g/mol. The purity is usually 95%.

3-Methoxycarbonylphenylboronic acid is a reactanct that has been involved in a variety of applications. For instance, it has been used in Suzuki-Miyaura cross-coupling, Iterative cross-coupling of boronate building blocks, cross-coupling with aryl/ alkenyl sulfonates, synthesis of symmetrical biaryls via CuCl catalyzed homocoupling, trifluoromethylation, and cyanation just to name a few of its many uses.

3-Methoxycarbonylphenylboronic acid is a boronate ligand that has been shown to have an interaction with the nitrogen atoms in amines. This compound is used for the Suzuki coupling reaction, which is a chemical reaction between an organoboron compound and an organic electrophile. 3-Methoxycarbonylphenylboronic acid has a helical structure that can be seen by FTIR spectroscopy and it has potent inhibitory activity., 99769-19-4.

Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics