In 2017,Barlaam, Bernard; Cosulich, Sabina; Fitzek, Martina; Germain, Herve; Green, Stephen; Hanson, Lyndsey L.; Harris, Craig S.; Hancox, Urs; Hudson, Kevin; Lambert-van der Brempt, Christine; Lamorlette, Maryannick; Magnien, Francoise; Ouvry, Gilles; Page, Ken; Ruston, Linette; Ward, Lara; Delouvrie, Benedicte published 《Discovery of a novel aminopyrazine series as selective PI3Kα inhibitors》.Bioorganic & Medicinal Chemistry Letters published the findings.Computed Properties of C4H7NO2S The information in the text is summarized as follows:
We report the discovery of a novel aminopyrazine series of PI3Kα inhibitors, designed by hybridizing two known scaffolds of PI3K inhibitors. We describe the progress achieved from the first compounds plagued with poor general kinase selectivity to compounds showing high selectivity for PI3Kα over PI3Kβ and excellent general kinase selectivity. This effort culminated with the identification of compound 5 displaying high potency and selectivity, and suitable physiochem. and pharmacokinetic properties for oral administration. In vivo, compound I showed good inhibition of tumor growth (86% tumor growth inhibition at 50 mg/kg twice daily orally) in the MCF7 xenograft model in mice. The results came from multiple reactions, including the reaction of Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1Computed Properties of C4H7NO2S)
Ethyl 2-amino-2-thioxoacetate(cas: 16982-21-1) 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.Computed Properties of C4H7NO2S
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