Anqi Zhang, Lan Yao and Ming An
Chem. Commun., 2017,53, 12826-12829
DOI:
10.1039/C7CC06843C,
Communication
The acid-labile behavior of di-substituted maleamic acid (DMA) and its equilibrium with di-substituted maleimide (DMI) are exploited to build an ultra acid-sensitive, small molecule prodrug that can be activated by tumor extracellular pH (pHe) in the range of 6.5–6.9. Such a DMA prodrug reversed the unfavorable pH-profile of doxorubicin (Dox), which may improve its therapeutic window.