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糖基卟啉化合物库的合成与生物评价。

Synthesis and biological evaluation of a library of glycoporphyrin compounds.

机构信息

School of Chemistry, Trinity Biomedical Sciences Institute, Trinity College Dublin, Ireland.

出版信息

Chemistry. 2012 Nov 12;18(46):14671-9. doi: 10.1002/chem.201202064. Epub 2012 Sep 27.

Abstract

A library of glycosylated porphyrins (glycoporphyrins) was prepared and the compounds were evaluated for their photodynamic therapy (PDT) activity against the oesophageal squamous-cell carcinoma cell line OE21 in vitro. A synthetic methodology was developed to allow incorporation of biologically active carbohydrates, including the histo-blood-group antigen trisaccharide Lewis(X), onto the porphyrin backbone. The effect of the carbohydrate group and substitution pattern on the PDT activity, cell uptake and subcellular localisation of the glycoporphyrin compounds is reported.

摘要

我们制备了糖基卟啉(glycoporphyrins)文库,并评估了它们对体外食管鳞状细胞癌细胞系 OE21 的光动力疗法(PDT)活性。我们开发了一种合成方法,使包括组织血型抗原三糖 Lewis(X)在内的具有生物活性的碳水化合物能够与卟啉主链结合。本文报道了糖基化合物的糖基部分和取代模式对卟啉化合物的 PDT 活性、细胞摄取和亚细胞定位的影响。

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