Phthalocyanine-cRGD conjugate: synthesis, photophysical properties and in vitro biological activity for targeting photodynamic therapy

Abstract

An unsymmetrical phthalocyanine conjugated with an RGDyK moiety (6) was synthesized and characterized. Its photophysical properties, including electronic absorption, fluorescence emission (Φ_F = 0.20), singlet oxygen quantum yield (Φ_Δ = 0.63) and two-photon absorption cross section (TPACS) at different wavelengths were studied. The in vitro cell study data demonstrate that this Pc conjugate possesses significantly high cellular uptake toward the α_νβ₃ positive DU145 prostate cancer cells along with an efficient photocytotoxicity (IC₅₀ = 0.04 μM), showing this compound is one of the most promising photosensitizers for targeting photodynamic therapy (PDT) of cancer.