Lucas, Simon C. C.; Atkinson, Stephen J.; Chung, Chun-wa; Davis, Rob; Gordon, Laurie; Grandi, Paola; Gray, James J. R.; Grimes, Thomas; Phillipou, Alexander; Preston, Alex G.; Prinjha, Rab K.; Rioja, Inmaculada; Taylor, Simon; Tomkinson, Nicholas C. O.; Wall, Ian; Watson, Robert J.; Woolven, James; Demont, Emmanuel H. published their research in Journal of Medicinal Chemistry on August 12 ,2021. The article was titled 《Optimization of a Series of 2,3-Dihydrobenzofurans as Highly Potent, Second Bromodomain (BD2)-Selective, Bromo and Extra-Terminal Domain (BET) Inhibitors》.Name: 4,4-Diethoxybutan-1-amine The article contains the following contents:
Herein, a series of 2,3-dihydrobenzofurans have been developed as highly potent bromo and extra-terminal domain (BET) inhibitors with 1000-fold selectivity for the second bromodomain over the first bromodomain. Investment in the development of two orthogonal synthetic routes delivered inhibitors that were potent and selective but had raised in vitro clearance and suboptimal solubility Insertion of a quaternary center into the 2,3-dihydrobenzofuran core blocked a key site of metabolism and improved the solubility This led to the development of inhibitor I (GSK852): a potent, 1000-fold-selective, highly soluble compound with good in vivo rat and dog pharmacokinetics. In the part of experimental materials, we found many familiar compounds, such as 4,4-Diethoxybutan-1-amine(cas: 6346-09-4Name: 4,4-Diethoxybutan-1-amine)
4,4-Diethoxybutan-1-amine(cas: 6346-09-4) belongs to anime. Amines have a free lone pair with which they can coordinate to metal centers. Amine–metal bonds are weaker because amines are incapable of backbonding, but they are still important for sensing applications.While stronger than hydrogen bonds, amine–metal bonds are still weaker than both covalent and ionic bonds.Name: 4,4-Diethoxybutan-1-amine
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