4.5 Article

Hydrogean Peroxide Inducible Acid-Activatable Prodrug for Targeted Cancer Treatment

Journal

CHEMMEDCHEM
Volume 16, Issue 20, Pages 3231-3235

Publisher

WILEY-V C H VERLAG GMBH
DOI: 10.1002/cmdc.202100354

Keywords

hydrogen peroxide; MIDA; prodrug; cancer treatment; tumor environments

Funding

  1. Young Science and Technology Plan Project of Gansu Province [20JR5RA193]
  2. General Program of the Key Laboratory of Hexi Corridor Resources Utilization of Gansu Universities [XZ2003]
  3. PhD Start-up Foundation of Hexi University of China [KYQD2020010]

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MIDA boronates in conjunction with naphthalene-based fluorophores are suitable compounds for tumor diagnosis due to their stability, controlled drug release, and potential for precision therapeutics.
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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