The ‘click’ synthesis of new cytotoxic conjugate based on meso-arylporphyrin and Erlotinib

New phototherapeutic agents based on synthetic porphyrin- type tetrapyrroles and small-molecule-targeted tyrosine kinase inhibitor Erlotinib have been synthesized based on the scheme involving ‘click’ reaction between bis(4- azidophenyl)-containing zinc porphyrinate derivative and N-(3-ethynylphenylamino)-6,7-bis(2-methoxyethoxy)- quinazoline. The final compound and its precursors were tested as potential photosensitizers for targeted photo- dynamic therapy (PDT), the conjugate having shown photoinduced cytotoxicity IC₅₀ for NKE cells 0.86 ± 0.017 μm and for A431 cells 0.54 ± 0.011 μm.