Provided are a novel chlorin e6 derivative and pharmaceutically-acceptable salts thereof, a preparation method therefor, and an application thereof, relating to the technical field of pharmacy. The chlorin e6 derivative ether-based amino acid derivative comprises structural general formula I and an optical isomer of the structural general formula I. The preparation method is: etherifying 3-vinyl in chlorin e6, and producing peptide from 15-acetate carboxyl and amino acid. The chlorin e6 derivative ether-based amino acid derivative and pharmaceutically-acceptable salts thereof can be used as anti-tumor drugs of photodynamic therapy. As compared with Talaporfin which is the existing clinically-used photosensitizer, the novel chlorin e6 derivative has advantages of stronger anti-tumor activity and higher dark toxicity-phototoxicity ratio, and can be used for preparing novel anti-tumor drugs of the photodynamic therapy, including caner-treating drugs of photodynamic therapy, drugs for treating benign vascular diseases by the photodynamic therapy such as macular degeneration and nevus flammeus, as well as drugs for treating condyloma acuminate by the photodynamic therapy.
