Computed Properties of C6H13NOIn 2022 ,《Design, Synthesis, and Structure-Activity Relationship Optimization of Pyrazolopyrimidine Amide Inhibitors of Phosphoinositide 3-Kinase γ (PI3Kγ)》 appeared in Journal of Medicinal Chemistry. The author of the article were Mata, Guillaume; Miles, Dillon H.; Drew, Samuel L.; Fournier, Jeremy; Lawson, Kenneth V.; Mailyan, Artur K.; Sharif, Ehesan U.; Yan, Xuelei; Beatty, Joel W.; Banuelos, Jesus; Chen, Jie; Ginn, Elaine; Chen, Ada; Gerrick, Kimberline Y.; Pham, Amber T.; Wong, Kent; Soni, Divyank; Dhanota, Puja; Shaqfeh, Stefan G.; Meleza, Cesar; Narasappa, Nell; Singh, Hema; Zhao, Xiaoning; Jin, Lixia; Schindler, Ulrike; Walters, Matthew J.; Young, Stephen W.; Walker, Nigel P.; Leleti, Manmohan Reddy; Powers, Jay P.; Jeffrey, Jenna L.. The article conveys some information:
Phosphoinositide-3-kinase γ (PI3Kγ) is highly expressed in immune cells and promotes the production and migration of inflammatory mediators. The inhibition of PI3Kγ has been shown to repolarize the tumor immune microenvironment to a more inflammatory phenotype, thereby controlling immune suppression in cancer. Herein, we report the structure-based optimization of an early lead series of pyrazolopyrimidine isoindolinones, which culminated in the discovery of highly potent and isoform-selective PI3Kγ inhibitors with favorable drug-like properties. X-ray cocrystal structure anal., mol. docking studies, and detailed structure-activity relationship investigations resulted in the identification of the optimal amide and isoindolinone substituents to achieve a desirable combination of potency, selectivity, and metabolic stability. Preliminary in vitro studies indicate that inhibition of PI3Kγ with compound 56 results in a significant immune response by increasing pro-inflammatory cytokine gene expression in M1 macrophages. In the experimental materials used by the author, we found trans-4-Aminocyclohexanol(cas: 27489-62-9Computed Properties of C6H13NO)
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Aniline, ethanolamines, and several other amines are major industrial commodities used in making rubber, dyes, pharmaceuticals, and synthetic resins and fibres and for a host of other applications. Most of the numerous methods for the preparation of amines may be broadly divided into two groups: (1) chemical reduction (replacement of oxygen with hydrogen atoms in the molecule) of members of several other classes of organic nitrogen compounds and (2) reactions of ammonia or amines with organic compounds.Computed Properties of C6H13NO
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