前药
生物正交化学
四嗪
化学
小分子
组合化学
部分
化学选择性
有机化学
生物化学
催化作用
点击化学
作者
Kevin Neumann,Alessia Gambardella,Mark Bradley
出处
期刊:ChemBioChem
[Wiley]
日期:2019-01-16
卷期号:20 (7): 872-876
被引量:27
标识
DOI:10.1002/cbic.201800590
摘要
Abstract Traditionally, prodrug activation has been limited to enzymatic triggers or gross physiological aberrations, such as pH, that offer low selectivity and control over dosage. In recent years, the field of prodrug activation chemistry has been transformed by the use of bioorthogonal reactions that can be carried out under biological conditions at sub‐millimolar concentrations, with the tetrazine‐mediated inverse electron demand Diels–Alder reaction amongst the most recognised. Their high reaction rates, chemoselectivity and excellent biocompatibility make tetrazines ideal small molecules for activating prodrugs. Recently the tetrazine moiety has been used as a prodrug for a pyridazine thus broadening the scope of prodrug systems. This article discusses the concept of using tetrazines as small‐molecule activators for prodrugs, and provides an overview of tetrazine‐based prodrug systems, with a particular focus on the recently reported prodrug–prodrug activation strategy.
科研通智能强力驱动
Strongly Powered by AbleSci AI