Diels-Alder adducts of vinyl porphyrins: synthesis and in vivo photodynamic effect against a rat bladder tumor.

摘要: Benzoporphyrin derivatives have been proposed as potential photosensitizers for photodynamic therapy. We prepared a number of benzoporphyrin and tested their effect, in combination with red light, on the N-[4-(5-nitro-2-furyl)-2-thiazolyl]formamide (FANFT) induced rat bladder tumor (AY-27) transplanted into Fischer CDF(F344)/CrlBr rats. Tetracyanoethylene (TCNE) adducts showed very little activity, which may be attributable to poor uptake or chemical instability adduct under physiological conditions. However, dimethyl acetylenedicarboxylate (DMAD) greater cytotoxic effect than hematoporphyrin derivative similar activities metallopurpurins when same protocol.