前药
过氧化物
化学
药品
硼酸
结合
过氧化氢
癌症研究
癌症治疗
癌症
药理学
组合化学
生物化学
作者
Jun Liu,Jinhua Wang,Shuang Si,Jinyi Xu,Peng Xue
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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