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发现了包含利多卡因和苯甲脒(吡嗪-1-基)乙炔基衍生物的半夹心铱配合物,用于光动力疗法。

The discovery of half-sandwich iridium complexes containing lidocaine and (pyren-1-yl)ethynyl derivatives of phenylcyanamide ligands for photodynamic therapy.

机构信息

School of Chemistry, National University of Ireland, Galway, University Road, Galway, Ireland.

出版信息

Dalton Trans. 2017 Jun 6;46(22):7242-7252. doi: 10.1039/c7dt01091e.

DOI:10.1039/c7dt01091e
PMID:28534895
Abstract

The successful design, synthesis, characterization, photophysical properties and anticancer mechanistic studies of a series of half-sandwich cyclopentadienyl iridium(iii) complexes of the type Cp*Ir(LC)(L1), 1, and Cp*Ir(LC)(L2), 2, in which Cp* = pentamethylcyclopentadienyl, L1 = 4-(pyren-10-yl)ethynyl-phenylcyanamide, L2 = 4'-(pyren-10-yl)ethynyl-4-cyanamidobiphenyl, and LC = lidocaine, are reported for their application as photodynamic therapy (PDT) agents. The DNA binding, DNA photocleavage, cellular uptake, and apoptosis of the complexes have also been studied.

摘要

报道了一系列半夹心环戊二烯基铱(III)配合物Cp*Ir(LC)(L1),1 和 Cp*Ir(LC)(L2),2 的成功设计、合成、表征、光物理性质和抗癌机制研究,其中 Cp* = 五甲基环戊二烯基,L1 = 4-(芘-10-基)乙炔基-苯甲腈酰胺,L2 = 4'-(芘-10-基)乙炔基-4-氰基联苯,LC = 利多卡因,它们被用作光动力疗法 (PDT) 试剂。还研究了配合物的 DNA 结合、DNA 光解、细胞摄取和细胞凋亡。

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