Abstract

A series of novel, highly symmetrical phthalocyanines bearing eight peptide residues has been prepared by microwave-­assisted Cu(I)-catalyzed 1,3-dipolar cycloaddition (‘click’ reaction). Water-soluble conjugates were obtained after straightforward deprotection of the amine and amide functionalities. The phthalocyanine conjugates were found to be nontoxic along the whole concentration range, which makes them promising photosensitizers for therapeutic use.

A series of novel, highly symmetrical phthalocyanines bearing eight peptide residues has been prepared by microwave-­assisted Cu(I)-catalyzed 1,3-dipolar cycloaddition (‘click’ reaction). Water-soluble conjugates were obtained after straightforward deprotection of the amine and amide functionalities. The phthalocyanine conjugates were found to be nontoxic along the whole concentration range, which makes them promising photosensitizers for therapeutic use.

中文翻译：

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微波辅助合成的三唑连接的酞菁-肽缀合物作为光动力疗法的潜在光敏剂。

摘要

通过微波辅助Cu（I）催化的1,3-偶极环加成反应（“点击”反应），制备了一系列带有八个肽残基的新型，高度对称的酞菁。在胺和酰胺官能团直接脱保护后获得水溶性缀合物。发现酞菁缀合物在整个浓度范围内是无毒的，这使其成为有前途的光敏剂以用于治疗。

通过微波辅助Cu（I）催化的1,3-偶极环加成反应（“点击”反应），制备了一系列带有八个肽残基的新型，高度对称的酞菁。在胺和酰胺官能团直接脱保护后获得水溶性缀合物。发现酞菁缀合物在整个浓度范围内是无毒的，这使其成为有前途的光敏剂以用于治疗。