Novel chlorophyll a derivatives with ester-linked galactose fragments for photodynamic therapy and fluorescence diagnostics of cancer

Abstract

In the present work, a number of chlorophyll [Formula: see text] derivatives were synthetized with galactose fragments with an ester bond between macrocycle and carbohydrate fragments. It showed that synthesized compounds fluoresce intensely inside HeLa cells, which enable these compounds to be considered as potential diagnostic agents and indicates their ability to remain in the cell in an unassociated photoactive state — a necessary condition for the realization of a photodynamic action. It was determined that while all conjugates had comparable photoinduced toxicities, the conjugate with phorbin macrocycle fragment had a much lower dark toxicity, which corresponds to the trends noted earlier. In terms of a therapeutic window, conjugate significantly exceeds similar derivatives of chlorin [Formula: see text] and is the most promising for further research.