Synthesis of a porphyrin with histidine-like chelate: an efficient path towards molecular PDT/SPECT theranostics
作者:Steven Y. Yap、Huguette Savoie、Isaline Renard、Benjamin P. Burke、Harry C. Sample、Saul Michue-Seijas、Stephen J. Archibald、Ross W. Boyle、Graeme J. Stasiuk
DOI:10.1039/d0cc03958f
日期:——
The goal of “personalised” medicine has seen a growing interest in the development of theranostic agents. Bifunctional, and targeted-trifunctional, theranostic water-soluble porphyrins with a histidine-like chelating group have been synthesised via copper-catalysed azide–alkyne cycloaddition (CuAAC) “click” chemistry in high yield and purity. They are capable of photodynamic treatment and [99mTc(CO)3]+
“个性化”医学的目标已引起对治疗诊断试剂发展的兴趣。通过铜催化的叠氮化物-炔烃环加成反应(点击)化学合成了具有组氨酸样螯合基团的双功能和靶向三功能的治疗性水溶性卟啉,具有高收率和纯度。它们能够进行光动力处理和[ 99m Tc(CO)3 ] +络合,用于单光子发射计算机断层扫描(SPECT)成像,放射化学产率> 95%。在HT-29细胞,DU145和DU145-PSMA细胞系上评估了毒性和光毒性,靶向治疗药物对表达DU145-PSMA的细胞表现出更强的光毒性。