Photosensitization with anticancer agents. 18. Perylenequinonoid pigments as potential photodynamic therapeutic agents: preparation and photodynamic properties of amino-substituted hypocrellin derivatives.

Perylenequinonoid pigments have demonstrated several photodynamic therapeutic advantages over the commonly used hematoporphyrin derivatives. Certain new amino-substituted hypocrellin B derivatives have been prepared, and both direct and reductive aminations of hypocrellin B are described. The photophysical and photochemical properties of the amino-substituted hypocrellin B derivatives were investigated, and their significantly enhanced red absorptivities and strong 1O2-generating functions qualify them as promising photodynamic therapeutic agents. In addition, the superoxide anion radical was also determined to be implicated in the photosensitization of the amino-substituted hypocrellin B derivatives.