Discovery of novel Akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma cells was written by Yu, Meng;Zeng, Minghui;Pan, Zhaoping;Wu, Fengbo;Guo, Li;He, Gu. And the article was included in European Journal of Medicinal Chemistry in 2020.Application of 587-88-2 This article mentions the following:
A series of thieno[2,3-d]pyrimidine derivatives I (X = O, CH2, NR1, Z = CH2; X = CH2, Z = nothing; R1 = Me, cyclopropyl, PhCH2, Me2NCO, etc.; R2 = 4-BrC6H4, 4-MeC6H4, 2-ClC6H4, etc.; R3 = Et, i-Pr, cyclohexyl, etc.) were designed, synthesized and evaluated as novel AKT1 inhibitors. In vitro antitumor assay results showed that compounds I (X = CH2; Z = nothing; R2 = 4-ClC6H4; R3 = Et, n-Bu, cyclopentyl, cyclohexyl) and I (X = CH2; Z = nothing; R2 = 4-BrC6H4; R3 = i-Pr) potently suppressed the enzymic activities of AKT1 and inhibited the proliferation of HepG2, Hep3B, Huh-7 and SMMC-7721 cancer cell lines. Among these derivatives, the compound I [X = CH2; Z = nothing; R2 = 4-ClC6H4; R3 = cyclopentyl; (II)] demonstrated the best inhibitory activities on AKT1 (IC50 = 0.034娓璏) and Huh-7 cell (IC50 = 0.076娓璏). A panel of biol. assays showed that compound II suppressed the cellular proliferation of Huh-7 through Akt/mTOR signaling pathway mediated autophagy mechanism. Furthermore, the antitumor capacity of II was validated in the s.c. Huh-7 xenograft models. Together, these results demonstrated that a novel small-mol. Akt1 inhibitor induces autophagy associated death in hepatocellular carcinoma, which may afforded a potential drug candidate for targeted cancer therapy. In the experiment, the researchers used many compounds, for example, Ethyl 2-(4-fluorophenyl)acetate (cas: 587-88-2Application of 587-88-2).
Ethyl 2-(4-fluorophenyl)acetate (cas: 587-88-2) belongs to esters. Esters are widespread in nature and are widely used in industry. In nature, fats are in general triesters derived from glycerol and fatty acids. Esters are responsible for the aroma of many fruits. Acyl chlorides and acid anhydrides alcoholysis is another way to produce esters. Acyl chlorides and acid anhydrides react with alcohols to produce esters. Anydrous conditions are recommended since both acyl chlorides and acid anhydrides react with water.Application of 587-88-2
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Ester – an overview | ScienceDirect Topics