4.8 Article

A New Prodrug-Derived Ratiometric Fluorescent Probe for Hypoxia: High Selectivity of Nitroreductase and Imaging in Tumor Cell

Journal

ORGANIC LETTERS
Volume 13, Issue 5, Pages 928-931

Publisher

AMER CHEMICAL SOC
DOI: 10.1021/ol102975t

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Funding

  1. Key New Drug Creation and Manufacturing Program [2009ZX09103-102]
  2. National High Technology Research and Development Program of China [2011AA10A207]
  3. National Basic Research Program of China [2010CB126100]
  4. China 111 Project [B07023]
  5. Shanghai Leading Academic Discipline Project [13507]

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Based on the hypoxia prodrug moiety of p-nitrobenzyl, a selective ratiometric fluorescent sensor (RHP) for the detection of microenvironment hypoxia was designed and synthesized. RHP can be selectively activated by bioreductive enzymes (NTR) and results in an evident blue to green fluorescent emission wavelength change in both solution phases and in cell lines, which might be the first fluorescent ratiometric probe for hypoxia in solid tumors.

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