Photodynamic Therapy (PDT) is one of the most recent approaches to treating tumors. Components of the PDT are photosensitizer (PS), oxygen and light, three non-toxic components that together can produce a toxic effect on the cells. For successful photodynamic therapy, it is essential to select a photosensitizer with good localization in cells. Porphyrins, tetrapyrrole macrocyclic compounds, due to their specific absorption and emission spectra, as well as the high yield of singlet oxygen, represent a highly efficient photosensitizers for PDT. Amphiphilic porphyrins are type of porphyrins that consist of hydrophilic part that allows better water solubility and hydrophobic part of the molecule that facilitates passing through the cell membrane. The synthesis of amphiphilic porphyrins is relatively simple, however purification of the compounds is often very difficult. In the synthesis of (oxidopyridyl)porphyrins conjugated with fatty acid chains, the main problem that occured was N-oxidation of the pyridyl nitrogens, and purification of the products. In this work, attempts for optimization of N-oxidation reactions of various 3-pyridylporphyrins and alternative pathways of synthesis of new (oxidopyridyl)porphyrin are described. Photophysical properties of the synthesized porphyrins were tested, and it was found that all synthesized pyridyporphyrins produce singlet oxygen in high yields. In the internalization test it was found that synthesized (oxido)pyridylporphyrin was not sufficiently soluble in water and buffers, and did not internalize into the cell probably due to the aggregation of the compound on the cell membrane. Also, it was shown that the compound is very toxic even with low intensity of light used for photoactivation, as shown by appearance of non-viable cells during the test.