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Photodiagnosis Photodyn Ther ; 11(4): 510-5, 2014 Dec.
Article in English | MEDLINE | ID: mdl-25102162

ABSTRACT

Improved photosensitizers for use in photomedicine must possess good water-solubility and optimal photophysical properties. Phosphorus(V) porphyrins fulfill these criteria and are a class of porphyrins with significant potential applications in phototherapy. Five phosphorus(V) porphyrins bearing alkyl substituents have been synthesized. Reasonable to good yields were obtained for all P(V) insertions and all compounds underwent biological evaluation for their PDT activity on two esophageal cancer cell lines, OE33 and SKGT-4. Their cellular uptake was investigated using a high content screening method. Notably, three compounds displayed good uptake and using the MTS cell proliferation assay, two were shown to have photocytotoxicity comparable to mTHPC (Temoporfin(®)) with IC50 values of 6.5 and 5.5 µM.


Subject(s)
Esophageal Neoplasms/drug therapy , Esophageal Neoplasms/metabolism , Porphyrins/pharmacokinetics , Porphyrins/therapeutic use , Apoptosis/drug effects , Apoptosis/radiation effects , Cell Line, Tumor , Cell Proliferation/drug effects , Cell Proliferation/radiation effects , Cell Survival/drug effects , Cell Survival/radiation effects , Esophageal Neoplasms/pathology , Humans , Light , Photochemotherapy , Photosensitizing Agents/chemical synthesis , Photosensitizing Agents/pharmacokinetics , Photosensitizing Agents/therapeutic use , Porphyrins/chemical synthesis , Solubility , Treatment Outcome , Water/chemistry
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