Structure‐Photodynamic Activity Relationships of a Series of 4‐Substituted Zinc Phthalocyanines

摘要: Radioiodinated zinc phthalocyanine including [125I]ZnPcI4 and differently sulfonated [65Zn]ZnPcS (ZnPcS4, ZnPcS3, ZnPcS2 ZnPcS1.75, a mixture of adjacent di 25% mono) were prepared in order to study cell uptake release kinetics EMT-6 cells. The same compounds evaluated for their vitro phototoxicity the biological parameters compared partition coefficients arrive at quantitative structure-activity relationships (QSAR). At 1 microM 1% serum, 37 degrees C, all dyes showed rapid during first hour followed by slow accumulation phase. After 24 h, highest cellular concentration was observed with lipophilic ZnPcI4, amphiphilic ZnPcS1.75. hydrophilic ZnPcS4 ZnPcS3 lower uptake. Dye from dye-loaded cells incubation dye-free medium could reach up 60% shown depend mainly on amount drug incorporated rather than type compound. These results suggest that care should be taken interpreting dye toxicity data, which involve manipulations medium, particularly vitro-in vivo protocols. survival after h or serum exposure red light assessed means colorimetric 3-(4,5-dimethylthiazol-2-yl)-diphenyl-tetrazolium bromide (MTT) assay. Photocytotoxicities correlated inversely tendencies aggregate. Increased also activities, except but little phototoxicity. QSAR between log (phosphate-buffered saline n-octanol) gave parabola optimal values corresponding ZnPcS2.