A number of porphyrin derivatives based on hematoporphyrin, 5,10,15,20-tetrasubstituted porphyrins, phthalocyanines, and naphthalocyanines were prepared either as low-molecular compounds or bonded with methoxypoly(ethylene glycol) or attached to silica of low surface area. The low-molecular weight and the polymer-bonded porphyrins exhibit comparable triplet lifetimes and activities in the photosensitized formation of singlet oxygen. For photon-induced processes, the monomeric state of sensitizers is fundamentally important. The porphyrins have been investigated as sensitizers for photooxidation of thiolates and sulfides, which occurs via singlet oxygen, and, therefore, is much more efficient than the corresponding catalytic dark oxidation. Polymer-bonded porphyrins and long-wavelength absorbing naphthalocyanines incorporated in liposomes exhibit in vivo high accumulation in tumor tissues. Under irradiation, singlet oxygen is produced, and efficient phototherapeutic effects are observed, which may be used for photodynamic cancer therapy.