Application of 27489-62-9In 2021 ,《Template-Hopping Approach Leads to Potent, Selective, and Highly Soluble Bromo and Extraterminal Domain (BET) Second Bromodomain (BD2) Inhibitors》 appeared in Journal of Medicinal Chemistry. The author of the article were Aylott, Helen E.; Atkinson, Stephen J.; Bamborough, Paul; Bassil, Anna; Chung, Chun-wa; Gordon, Laurie; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Hayhow, Thomas G.; Messenger, Cassie; Mitchell, Darren; Phillipou, Alexander; Preston, Alex; Prinjha, Rab K.; Rianjongdee, Francesco; Rioja, Inmaculada; Seal, Jonathan T.; Wall, Ian D.; Watson, Robert J.; Woolven, James M.; Demont, Emmanuel H.. The article conveys some information:
A number of reports have recently been published describing the discovery and optimization of bromo and extraterminal inhibitors which are selective for the second bromodomain (BD2); these include our own work toward GSK046 and GSK620. This paper describes our approach to mitigating the genotoxicity risk of GSK046 by replacement of the acetamide functionality with a heterocyclic ring. This was followed by a template-hopping and hybridization approach, guided by structure-based drug design, to incorporate learnings from other BD2-selective series, optimize the vector for the amide region, and explore the ZA cleft, leading to the identification of potent, selective, and bioavailable compounds GSK452, GSK737, and GSK217. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Application of 27489-62-9)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Reduction of nitro compounds, RNO2, by hydrogen or other reducing agents produces primary amines cleanly (i.e., without a mixture of products), but the method is mostly used for aromatic amines because of the limited availability of aliphatic nitro compounds. Reduction of nitriles and oximes (R2C=NOH) also yields primary amines.Application of 27489-62-9
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