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New Photosensitizers for Photodynamic Therapy: Combined Effect of Metallopurpurin Derivatives and Light on Transplantable Bladder Tumors¹

Department of Chemistry, University of Toledo, and Department of Surgery/Urology, Medical College of Ohio, Toledo, Ohio 43606

A series of metallopurpurins was tested for their photodynamic activity against transplantable N-[4-(5-nitro-2-furyl)-2-thiazoyl]formamide-induced urothelial tumors growing in male Fischer CDF (F344/CrlBR) rats. Histological examination of tumors in animals treated with the metallopurpurins and red light (>590 nm, 360 J/cm²) revealed tumor necrosis 24 h after completion of therapy. Control tumors showed no histological change.

In 30-day tumor regrowth studies, 70% of animals treated with the metallopurpurin derivative SnET2 were free of tumors while 50% of the animals treated with the free-base purpurin ET2 were free of tumor.

Metallopurpurins have intense absorptions in the red region of the visible spectrum, a region with good tissue penetration. The metallopurpurins are easily prepared from the corresponding purpurins with a high degree of purity. This study demonstrates the potential of these photosensitizers for photodynamic cancer therapy.

¹ Supported in part by PHS Grants R01 CA43006 and R23 CA38754 awarded by the National Cancer Institute, Department of Health and Human Services.

² To whom all correspondence should be addressed, at Department of Chemistry, University of Toledo, 2801 W. Bancroft Street, Toledo, OH 43606.

Received 1/20/87. Revised 7/30/87. Accepted 10/ 7/87.

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