Design and stereoselective synthesis of novel β-lactone and β-lactams as potent anticancer agents on breast cancer cells
作者:Mahnoosh Rashidi、Mohammad Reza Islami、Saeed Esmaeili-Mahani
DOI:10.1016/j.tet.2017.12.044
日期:2018.2
To produce a novel class of anticancer compounds, an efficient method for synthesizing novel β-lactone and β-lactam frameworks was developed based on the reaction of a new ketene with C=O and C=N bonds. Functionalized 2-azetidinones were efficiently synthesized by employing 2,4-dichlorophenoxylketene, which was generated in situ. The reaction of the ketene with aldehydes was not successful and in all
为了生产一类新型的抗癌化合物,基于新的烯酮与C = O和C = N键的反应,开发了一种有效的合成新型β-内酯和β-内酰胺骨架的方法。通过使用原位生成的2,4-二氯苯氧基乙烯酮,可以有效地合成功能化的2-氮杂环丁酮。乙烯酮与醛的反应不成功,并且在所有情况下,除了4-硝基苯甲醛以外,都获得了乙烯酮的重排二聚体作为内酯。研究了所有新的β-内酰胺和内酯对乳腺癌细胞的抗癌活性。所有新合成的化合物均显示出潜在的抗癌活性,这可能保证其将来在中度化疗中的应用。