Abstract
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.
Publication types
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Comparative Study
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Research Support, U.S. Gov't, P.H.S.
MeSH terms
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Animals
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Dose-Response Relationship, Radiation
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Drug Screening Assays, Antitumor
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Fluorine / chemistry*
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Fluorine / pharmacokinetics
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Fluorine / pharmacology*
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Fluorine / therapeutic use
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Light
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Mice
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Mice, Inbred C3H
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Molecular Structure
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Neoplasm Transplantation
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Photochemotherapy / methods*
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Photosensitizing Agents / chemistry*
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Photosensitizing Agents / pharmacokinetics
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Photosensitizing Agents / pharmacology*
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Photosensitizing Agents / therapeutic use
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Porphyrins / chemistry*
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Porphyrins / pharmacokinetics
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Porphyrins / pharmacology*
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Porphyrins / therapeutic use
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Sarcoma, Experimental / drug therapy
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Sarcoma, Experimental / metabolism
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Sarcoma, Experimental / pathology
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Time Factors
Substances
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Photosensitizing Agents
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Porphyrins
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Fluorine