The author of 《Identification of Novel, Potent, and Orally Available GCN2 Inhibitors with Type I Half Binding Mode》 were Fujimoto, Jun; Kurasawa, Osamu; Takagi, Terufumi; Liu, Xin; Banno, Hiroshi; Kojima, Takuto; Asano, Yasutomi; Nakamura, Akito; Nambu, Tadahiro; Hata, Akito; Ishii, Tsuyoshi; Sameshima, Tomoya; Debori, Yasuyuki; Miyamoto, Maki; Klein, Michael G.; Tjhen, Richard; Sang, Bi-Ching; Levin, Irena; Lane, Scott Weston; Snell, Gyorgy P.; Li, Ke; Kefala, Georgia; Hoffman, Isaac D.; Ding, Steve C.; Cary, Douglas R.; Mizojiri, Ryo. And the article was published in ACS Medicinal Chemistry Letters in 2019. COA of Formula: C6H13NO The author mentioned the following in the article:
General control nonderepressible 2 (GCN2) is a master regulator kinase of amino acid homeostasis and important for cancer survival in the tumor microenvironment under amino acid depletion. We initiated studies aiming at the discovery of novel GCN2 inhibitors as first-in-class antitumor agents and conducted modification of the substructure of sulfonamide derivatives with expected type I half binding on GCN2. Our synthetic strategy mainly corresponding to the αC-helix allosteric pocket of GCN2 led to significant enhancement in potency and a good pharmacokinetic profile in mice. In addition, compound 6d, which showed slow dissociation in binding on GCN2, demonstrated antiproliferative activity in combination with the asparagine-depleting agent asparaginase in an acute lymphoblastic leukemia (ALL) cell line, and it also displayed suppression of GCN2 pathway activation with asparaginase treatment in the ALL cell line and mouse xenograft model. In addition to this study using trans-4-Aminocyclohexanol, there are many other studies that have used trans-4-Aminocyclohexanol(cas: 27489-62-9COA of Formula: C6H13NO) was used in this study.
trans-4-Aminocyclohexanol(cas: 27489-62-9) belongs to anime. Hydrogen peroxide (H2O2) and peroxy acids generally add an oxygen atom to the nitrogen of amines. With primary amines, this step is normally followed by further oxidation, leading to nitroso compounds, RNO, or nitro compounds, RNO2. Secondary amines are converted to hydroxylamines, R2NOH, and tertiary amines to amine oxides, R3NO.COA of Formula: C6H13NO
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