Electric Literature of C6H13NOIn 2021 ,《Fragment-based Scaffold Hopping: Identification of Potent, Selective, and Highly Soluble Bromo and Extra Terminal Domain (BET) Second Bromodomain (BD2) Inhibitors》 was published in Journal of Medicinal Chemistry. The article was written by Seal, Jonathan T.; Atkinson, Stephen J.; Bamborough, Paul; Bassil, Anna; Chung, Chun-wa; Foley, James; Gordon, Laurie; Grandi, Paola; Gray, James R. J.; Harrison, Lee A.; Kruger, Ryan G.; Matteo, Jeanne J.; McCabe, Michael T.; Messenger, Cassie; Mitchell, Darren; Phillipou, Alex; Preston, Alex; Prinjha, Rab K.; Rianjongdee, Francesco; Rioja, Inmaculada; Taylor, Simon; Wall, Ian D.; Watson, Robert J.; Woolven, James M.; Wyce, Anastasia; Zhang, Xi-Ping; Demont, Emmanuel H.. The article contains the following contents:
The profound efficacy of pan-BET inhibitors is well documented, but these epigenetic agents have shown pharmacol.-driven toxicity in oncol. clin. trials. The opportunity to identify inhibitors with an improved safety profile by selective targeting of a subset of the eight bromodomains of the BET family has triggered extensive medicinal chem. efforts. In this article, we disclose the identification of potent and selective drug-like pan-BD2 inhibitors such as pyrazole 23 (GSK809) and furan 24 (GSK743) that were derived from the pyrrole fragment 6. We transpose the key learnings from a previous pyridone series (GSK620 2 as a representative example) to this novel class of inhibitors, which are characterized by significantly improved solubility relative to our previous research. The experimental process involved the reaction of trans-4-Aminocyclohexanol(cas: 27489-62-9Electric Literature of C6H13NO)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Electric Literature of C6H13NO
Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts