Photodynamictherapy (PDT) using a photo sensitizing agent and several light sources has been shown to have nonspecific and noninvasive effects on superficial cancers. Phthalocyanine (Pc) derivatives as novel photosens...Photodynamictherapy (PDT) using a photo sensitizing agent and several light sources has been shown to have nonspecific and noninvasive effects on superficial cancers. Phthalocyanine (Pc) derivatives as novel photosensitizers, trifluoroethoxy-coatedzinc Pcconjugated with β-cyclodextrin (βCD-4TFEO-Pc) was synthesized and its photodynamic effect in vitro and in vivo was evaluated. βCD-4TFEO-Pc alone was completely non-cytotoxic even at high concentrations, and showed excellentphotodynamic effects in B16-F10 and HT-1080 celllines. The in vivo antitumor effect of βCD-4TFEO-Pc against B16-F10 cells transplanted on to the chorioallantoic membranes of chickembryos was 52.7%, but that of laserirradiation alone and photosensitizer alone was 2 (50 mW). These data suggest that βCD-4TFEO-Pc is a useful photosensitizer for the treatment of superficial cancers. If a high-power LED with optimal wavelength is developed, excellent treatment of superficial cancers could be achieved by applying βCD-4TFEO-Pc for PDT.展开更多
A novel iodonium-ylide compound 2 that appends a trifluoromethylthio （SCF3） group is disclosed as a new, shelf-stable electrophilic trifluoromethylation reagent. Unlike known shelf-stable electrophilic trifluorometh...A novel iodonium-ylide compound 2 that appends a trifluoromethylthio （SCF3） group is disclosed as a new, shelf-stable electrophilic trifluoromethylation reagent. Unlike known shelf-stable electrophilic trifluoromethylation reagents, 2 has a stable SCF3 group which is activated by appending iodonium ylide under copper catalysis via sul- fonium ylide to generate a cationic trifluoromethyl （CF3） species. Reagent 2 was found to be an efficient electro- philic trifluoromethylation reagent for a wide range of silyl enol ethers 3 under copper catalysis. Cyclic and acyclic a-trifiuoromethyl ketones 4 were obtained by reagent 2 in moderate to good yields. On the other hand, a difluoro- methylthio analogue 5 did not affect intermolecular transfer difluoromethylation to substrates. Instead, intramolecu- lar 1,4-migration proceeded similar to the Stevens rearrangement to provide 6 in 21% yield, independent of the presence of nucleophiles 3.展开更多
文摘Photodynamictherapy (PDT) using a photo sensitizing agent and several light sources has been shown to have nonspecific and noninvasive effects on superficial cancers. Phthalocyanine (Pc) derivatives as novel photosensitizers, trifluoroethoxy-coatedzinc Pcconjugated with β-cyclodextrin (βCD-4TFEO-Pc) was synthesized and its photodynamic effect in vitro and in vivo was evaluated. βCD-4TFEO-Pc alone was completely non-cytotoxic even at high concentrations, and showed excellentphotodynamic effects in B16-F10 and HT-1080 celllines. The in vivo antitumor effect of βCD-4TFEO-Pc against B16-F10 cells transplanted on to the chorioallantoic membranes of chickembryos was 52.7%, but that of laserirradiation alone and photosensitizer alone was 2 (50 mW). These data suggest that βCD-4TFEO-Pc is a useful photosensitizer for the treatment of superficial cancers. If a high-power LED with optimal wavelength is developed, excellent treatment of superficial cancers could be achieved by applying βCD-4TFEO-Pc for PDT.
文摘A novel iodonium-ylide compound 2 that appends a trifluoromethylthio （SCF3） group is disclosed as a new, shelf-stable electrophilic trifluoromethylation reagent. Unlike known shelf-stable electrophilic trifluoromethylation reagents, 2 has a stable SCF3 group which is activated by appending iodonium ylide under copper catalysis via sul- fonium ylide to generate a cationic trifluoromethyl （CF3） species. Reagent 2 was found to be an efficient electro- philic trifluoromethylation reagent for a wide range of silyl enol ethers 3 under copper catalysis. Cyclic and acyclic a-trifiuoromethyl ketones 4 were obtained by reagent 2 in moderate to good yields. On the other hand, a difluoro- methylthio analogue 5 did not affect intermolecular transfer difluoromethylation to substrates. Instead, intramolecu- lar 1,4-migration proceeded similar to the Stevens rearrangement to provide 6 in 21% yield, independent of the presence of nucleophiles 3.
