吡啶
动力学分辨率
细胞毒性
化学
产量(工程)
转化(遗传学)
戒指(化学)
盐(化学)
酶
双环分子
癌细胞系
组合化学
立体化学
有机化学
癌细胞
体外
材料科学
生物化学
癌症
生物
催化作用
对映选择合成
基因
冶金
遗传学
作者
Carlos A. M. Afonso,João R. Vale,Milene A. G. Fortunato,Késsia H. S. Andrade,Filipa Siopa
标识
DOI:10.26434/chemrxiv-2022-314m3
摘要
Agelastatin alkaloids were synthesized through early-stage construction of the synthetically challenging C ring via photochemical transformation of pyridinium salts. Kinetic enzymatic resolution of bicyclic vinyl aziridines allowed the synthesis of (-)-agelastatin A in 4% yield over 12 steps. The cytotoxicity of (±)-agelastatin A and two N3-derivates were tested against a series of cancer cell lines to evaluate the impact of N3-substituition of the biological activity of agelastatin derivatives and corroborated the importance of unsubstituted N3 in the cytotoxicity of (-)-agelastatin A.
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