Hydrogen peroxide responsive theranostics for cancer-selective activation of DNA alkylators and real-time fluorescence monitoring in living cells.

ABSTRACT: Triple negative breast cancer (TNBC) is a notoriously difficult disease to treat, and many of the existing TNBC chemotherapeutics lack tumor selectivity and the capability for simultaneously visualizing and monitoring their own activity in the biological context. However, TNBC cells have been known to generate high levels of reactive oxygen species (ROS), such as hydrogen peroxide (H₂O₂). To this end, three novel small molecule theranostics 1a, 1c, and 2 consisting of both H₂O₂-responsive nitrogen mustard prodrug and profluorophore character have been designed, synthesized, and evaluated as targeted cancer therapeutics and bioimaging agents. The three theranostics comprise of boronate esters that deactivate nitrogen mustard functional groups and

SUBMITTER: Saxon E 

PROVIDER: S-EPMC12328069 | biostudies-literature | 2024 Oct

REPOSITORIES: biostudies-literature