前药
过氧化物
化学
药品
硼酸
结合
癌症治疗
癌症
药理学
组合化学
生物化学
有机化学
医学
数学
内科学
数学分析
作者
Jun Liu,Jinhua Wang,Shuang Si,Jinyi Xu,Peng Xue
出处
期刊:ChemMedChem
[Wiley]
日期:2021-07-21
卷期号:16 (20): 3231-3235
被引量:4
标识
DOI:10.1002/cmdc.202100354
摘要
Because some of the potentially most useful boronic acids are inherently unstable in blood plasma and exhibit poor selective retention in tumours, 2-heterocyclic N-methyliminodiacetic acid (MIDA) boronates provide a stable, spacious and highly effective harbor for prodrug conjugates. Herein we report MIDA boronates in conjunction with naphthalene-based fluorophores as suitable compounds for tumour diagnosis by virtue of their remarkable specificity and uniform benchtop stability. The shielding group was found to be effective at imparting stability under physiological conditions (pH 7.4), with rapid release of the drug upon exposure to the acidic microenvironment of the tumor. This approach significantly enhanced the efficiency of drug release and was found to exhibit fewer side effects, thus indicating its great potential for precision therapeutics.
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