A first comparative study of purpurinimide-based fluorinated vs. nonfluorinated photosensitizers for photodynamic therapy.
A first report on the synthesis and comparative in vitro-in vivo photosensitizing efficacy of various fluorinated and the corresponding nonfluorinated, purpurinimide-based photosensitizers is discussed. In preliminary in vivo screening, compared with the nonfluorinated analogs, purpurinimides bearing trifluoromethyl substituents showed enhanced photosensitizing efficacy. Among compounds (isomers) with similar lipophilicity, the position of the substituents was found to play a decisive role in biological efficacy.
Gryshuk
Amy L
AL
Photodynamic Therapy Center, Roswell Park Cancer Institute, Buffalo, NY 14263, USA.
Graham
Andrew
A
Pandey
Suresh K
SK
Potter
William R
WR
Missert
Joseph R
JR
Oseroff
Allan
A
Dougherty
Thomas J
TJ
Pandey
Ravindra K
RK
D000818:Animals; D004307:Dose-Response Relationship, Radiation; D004354:Drug Screening Assays, Antitumor; D005461:Fluorine / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D008027:Light; D051379:Mice; D008809:Mice, Inbred C3H; D015394:Molecular Structure; D009368:Neoplasm Transplantation; D010778:Photochemotherapy / Q000379:methods*; D017319:Photosensitizing Agents / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D011166:Porphyrins / Q000737:chemistry* / Q000493:pharmacokinetics / Q000494:pharmacology* / Q000627:therapeutic use; D012513:Sarcoma, Experimental / Q000188:drug therapy / Q000378:metabolism / Q000473:pathology; D013997:Time Factors
D017319:Photosensitizing Agents; D011166:Porphyrins; D005461:Fluorine