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新型轴向取代硅(IV)酞菁及其牛血清白蛋白缀合物的制备与体外光动力活性

Preparation and in vitro photodynamic activities of novel axially substituted silicon (IV) phthalocyanines and their bovine serum albumin conjugates.

作者信息

Jiang Xiong-Jie, Huang Jian-Dong, Zhu Yu-Jiao, Tang Fen-Xiang, Ng Dennis K P, Sun Jian-Cheng

机构信息

College of Chemistry and Chemical Engineering, Institute of Research on Functional Materials, Fuzhou University, Fuzhou 350002, China.

出版信息

Bioorg Med Chem Lett. 2006 May 1;16(9):2450-3. doi: 10.1016/j.bmcl.2006.01.075. Epub 2006 Feb 7.

DOI:10.1016/j.bmcl.2006.01.075
PMID:16464589
Abstract

Two novel axially substituted phthalocyanines, namely bis(4-(4-acetylpiperazine)phenoxy)phthalocyaninatosilicon (IV) (1) and its N-methylated derivative 2, have been synthesized. The dicationic phthalocyanine 2 is non-aggregated in water and exhibits good photophysical properties. The non-covalent BSA conjugates of these compounds have also been prepared. Compound 2 and the conjugate 2-BSA show extremely high photodynamic activities toward B16 melanoma cancer cell lines. The corresponding 50% growth-inhibitory (IC50) ratios are 33 and 38 nM, respectively.

摘要

两种新型轴向取代的酞菁化合物,即双(4-(4-乙酰基哌嗪)苯氧基)酞菁硅(IV)(1)及其N-甲基化衍生物2,已被合成。二价阳离子酞菁2在水中不聚集,并表现出良好的光物理性质。这些化合物的非共价牛血清白蛋白(BSA)缀合物也已制备出来。化合物2和缀合物2-BSA对B16黑色素瘤癌细胞系表现出极高的光动力活性。相应的50%生长抑制(IC50)率分别为33和38 nM。

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