TY - JOUR
T1 - Folic acid conjugates with photosensitizers for cancer targeting in photodynamic therapy
T2 - Synthesis and photophysical properties
AU - Stallivieri, Aurélie
AU - Colombeau, Ludovic
AU - Jetpisbayeva, Gulim
AU - Moussaron, Albert
AU - Myrzakhmetov, Bauyrzhan
AU - Arnoux, Philippe
AU - Acherar, Samir
AU - Vanderesse, Régis
AU - Frochot, Céline
N1 - Publisher Copyright:
© 2016 Elsevier Ltd
PY - 2017
Y1 - 2017
N2 - Recent researches in photodynamic therapy have focused on novel techniques to enhance tumour targeting of anticancer drugs and photosensitizers. Coupling a photosensitizer with folic acid could allow more effective targeting of folate receptors which are over-expressed on the surface of many tumour cells. In this study, different folic acid–OEG-conjugated photosensitizers were synthesized, characterized and their photophysical properties were evaluated. The introduction of an OEG does not significantly improve the hydrophilicity of the FA–porphyrin. All the FA-targeted photosensitizers present good to very good photophysical properties. The best one appears to be Ce6. Molar extinction coefficient, fluorescence and singlet oxygen quantum yields were determined and were compared to the corresponding photosensitizer alone.
AB - Recent researches in photodynamic therapy have focused on novel techniques to enhance tumour targeting of anticancer drugs and photosensitizers. Coupling a photosensitizer with folic acid could allow more effective targeting of folate receptors which are over-expressed on the surface of many tumour cells. In this study, different folic acid–OEG-conjugated photosensitizers were synthesized, characterized and their photophysical properties were evaluated. The introduction of an OEG does not significantly improve the hydrophilicity of the FA–porphyrin. All the FA-targeted photosensitizers present good to very good photophysical properties. The best one appears to be Ce6. Molar extinction coefficient, fluorescence and singlet oxygen quantum yields were determined and were compared to the corresponding photosensitizer alone.
KW - Cancer targeting
KW - Folic acid
KW - Photodynamic therapy
KW - Photosensitizers
KW - Singlet oxygen
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U2 - 10.1016/j.bmc.2016.10.004
DO - 10.1016/j.bmc.2016.10.004
M3 - Article
C2 - 27769669
AN - SCOPUS:85006041863
SN - 0968-0896
VL - 25
SP - 1
EP - 10
JO - Bioorganic and Medicinal Chemistry
JF - Bioorganic and Medicinal Chemistry
IS - 1
ER -
