Observations on the synthesis and in vivo photodynamic activity of some benzochlorins
| Autor: | Dimitris Skalkos, Rick W. Keck, George Maguire, Alan R. Morgan, Greta M. Garbo, Ashraf Rampersaud, Steven H. Selman |
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| Rok vydání: | 1992 |
| Předmět: |
Formamide
Radiation-Sensitizing Agents Magnetic Resonance Spectroscopy Porphyrins medicine.medical_treatment Photodynamic therapy Antineoplastic Agents Biochemistry Chemical synthesis chemistry.chemical_compound Structure-Activity Relationship In vivo medicine Animals Photosensitizer Physical and Theoretical Chemistry Molecular Structure General Medicine Combinatorial chemistry Rats Inbred F344 Rats chemistry Photochemotherapy Urinary Bladder Neoplasms Derivative (chemistry) Prolonged treatment |
| Zdroj: | Photochemistry and photobiology. 55(1) |
| ISSN: | 0031-8655 |
| Popis: | An improved synthesis of benzochlorins is reported. Demetallation of the meso-hydroxyme- thylvinyl derivative of octaethylporphyrin, followed by treatment with sulfuric acid results in cyclization to generate the corresponding octaethylbenzochlorin in high yield. Prolonged treatment with acid generates the sulfonated derivative. These sensitizers were shown to be efficient photodynamic agents in vivo. Animals bearing a transplanted N-(4-(5-nitro-2-furyl)-2-thiazolyl}formamide induced urothelial tumor were treated with either the benzochlorin or its sulfonated derivative. Irradiation of tumors 24 h later resulted in a significant tumoricidal effect in a short term assay. We conclude that benzochlor- ins warrant further examination as potential agents for use in photodynamic therapy. |
| Databáze: | OpenAIRE |
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