Synthesis and cellular properties of a 131substituted chlorin e6-nevirapine conjugate

Abstract

The synthesis of a chlorin e6-nevirapine conjugate is reported, in which the nevirapine moiety is attached to the 131-position of chlorin e6 via a diethylene glycol linker. This conjugate was found to be nontoxic in the dark (IC[Formula: see text] > 200 [Formula: see text]M), but highly phototoxic (IC[Formula: see text] = 0.21 [Formula: see text]M at 1.5 J/cm[Formula: see text] toward human HEp2 cells. The chlorin e6-nevirapine conjugate accumulated within cells in multiple organelles, including the Golgi, lysosomes and mitochondria. On the other hand, nevirapine was found to be nontoxic to HEp2 cells.