Synthesis and biological evaluation of novel 1,4-benzodiazepin-3-one derivatives as potential antitumor agents against prostate cancer was written by Vezina-Dawod, Simon;Perreault, Martin;Guay, Louis-David;Gerber, Nicolas;Gobeil, Stephane;Biron, Eric. And the article was included in Bioorganic & Medicinal Chemistry in 2021.Recommanded Product: 2-Methoxyethylamine The following contents are mentioned in the article:
A novel tumor suppressing agent was discovered against PC-3 prostate cancer cells from the screening of a 1,4-benzodiazepin-3-one library. In this study, 96 highly diversified 2,4,5-trisubstituted 1,4-benzodiazepin-3-one derivatives were prepared by a two-step approach using sequential Ugi multicomponent reaction and simultaneous deprotection and cyclization to afford pure compounds bearing a wide variety of substituents. The most promising compound (I) showed a potent and selective antiproliferative activity against prostate cancer cell line PC-3 (GI50 = 10.2μM), but had no effect on LNCAP, LAPC4 and DU145 cell lines. The compound was initially prepared as a mixture of two diastereomers and after their separation by HPLC, similar antiproliferative activities against PC-3 cells were observed for both diastereomers (2S,5S: GI50 = 10.8μM and 2S,5R: GI50 = 7.0μM). Addnl., both diastereomers showed comparable stability profiles after incubation with human liver microsomes. Finally, in vivo evaluation of the hit compound with the chick chorioallantoic membrane xenograft assay revealed a good toxicity profile and significant antitumor activity after i.v. injection. This study involved multiple reactions and reactants, such as 2-Methoxyethylamine (cas: 109-85-3Recommanded Product: 2-Methoxyethylamine).
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.Recommanded Product: 2-Methoxyethylamine
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Ether – Wikipedia,
Ether | (C2H5)2O – PubChem