Synthesis of selective PAK4 inhibitors for lung metastasis of lung cancer and melanoma cells was written by Song, Peilu;Zhao, Fan;Li, Dahong;Qu, Jiqiang;Yao, Miao;Su, Yuan;Wang, Hanxun;Zhou, Miaomiao;Wang, Yujie;Gao, Yinli;Li, Feng;Zhao, Dongmei;Zhang, Fengjiao;Rao, Yu;Xia, Mingyu;Li, Haitao;Wang, Jian;Cheng, Maosheng. And the article was included in Acta Pharmaceutica Sinica B in 2022.Product Details of 109-85-3 The following contents are mentioned in the article:
The p21 activated kinase 4 (PAK4) is serine/threonine protein kinase that is critical for cancer progression. Guided by X-ray crystallog. and structure-based optimization, we report a novel subseries of C-3-substituted 6-ethynyl-1H-indole derivatives that display high potential and specificity towards group II PAKs. Among these inhibitors, compound 55 exhibited excellent inhibitory activity and kinase selectivity, displayed superior anti-migratory and anti-invasive properties against the lung cancer cell line A549 and the melanoma cell line B16. Compound 55 exhibited potent in vivo antitumor metastatic efficacy, with over 80% and 90% inhibition of lung metastasis in A549 or B16-BL6 lung metastasis models, resp. Further mechanistic studies demonstrated that compound 55 mitigated TGF-β1-induced epithelial-mesenchymal transition (EMT). This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Product Details of 109-85-3).
2-Methoxyethylamine (cas: 109-85-3) belongs to ethers. 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, including apples, durians, pears, bananas, pineapples, and strawberries. 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.Product Details of 109-85-3
Referemce:
Ether – Wikipedia,
Ether | (C2H5)2O – PubChem