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The compounds containing the tetrapyrolic macrocycle, that is, porphyrins and their derivatives, are known as scaffolds for anticancer photodynamic therapy agents (photosensitizers). However, porphyrins are exceptionally suit- able for chemical modifications; moreover, these compounds can preferentially accumulate in tumor cells. Multiple structural modifications allow for the design of agents capable of evoking the cytotoxicity per se, i.e., the compounds that kill tumor cells being administered alone. We analyze the modes and quantitative parameters of binding of por- phyrins and their derivatives to DNA, a major intracellular target important for the antitumor potency of chemothera- peutic drugs. In particular, a possibility to inhibit the DNA-dependent enzyme telomerase makes the tetrapyrrole-based compounds perspective as anticancer agents beyond their established role as photosensitizers.