In 2020 EUR J MED CHEM published article about LUNG-CANCER; METABOLISM; EXPRESSION; IDENTIFICATION; AZD7545 in [Xiang, Sichuan; Huang, Ding; He, Qiaolin; Li, Jie; Zhang, Shao-Lin; He, Yun] Chongqing Univ, Sch Pharmaceut Sci, Chongqing Key Lab Nat Prod Synth & Drug Res, Chongqing 401331, Peoples R China; [Tam, Kin Yip] Univ Macau, Fac Hlth Sci, Taipa, Macau, Peoples R China in 2020, Cited 26. The Name is 3-Methylbenzoic acid. Through research, I have a further understanding and discovery of 99-04-7. Application In Synthesis of 3-Methylbenzoic acid
Most cancer cells feature an altered glucose metabolism from oxidative phosphorylation to cytoplasmic glycolysis. Pyruvate dehydrogenase kinases (PDKs) and lactate dehydrogenase A (LDHA) play crucial roles in promotion of glycolysis, thus the inhibition of both enzymes is considered a promising strategy for developing of anticancer therapeutics. Herein, we describe the first discovery of series novel dual inhibitors targeting PDKs and LDHA. We identified 6 hits from a library database containing 485465 compounds through a high-throughput virtual screening assay. Hit-to-lead optimization enabled us to discover two compounds, namely 20e and 20k, which inhibited PDKs with IC50 values of 0.8, and 1.6 mu M, respectively, and inhibited LDHA with IC50 values of 0.15 and 0.7 mu M, respectively. Meanwhile, the two compounds reduced A549 cell proliferation with EC50 values of 13.2, and 15.7 mu M. Furthermore, 20e and 20k decreased the lactate formation, and increased oxygen consumption, suggesting the two compounds modulated the glucose metabolic pathways in cancer cells. (C) 2020 Elsevier Masson SAS. All rights reserved.
Application In Synthesis of 3-Methylbenzoic acid. About 3-Methylbenzoic acid, If you have any questions, you can contact Xiang, SC; Huang, D; He, QL; Li, J; Tam, KY; Zhang, SL; He, Y or concate me.
Reference:
Isothiazole – Wikipedia,
,Isothiazole – ScienceDirect.com