Synthesis and in Vitro Photodynamic Activities of Pegylated Distyryl Boron Dipyrromethene Derivatives

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• 作者：Hui He ; Pui-Chi Lo ; Sin-Lui Yeung ; Wing-Ping Fong ; Dennis K. P. Ng
• 刊名：Journal of Medicinal Chemistry
• 出版年：2011
• 出版时间：April 28, 2011
• 年：2011
• 卷：54
• 期：8
• 页码：3097-3102
• 全文大小：844K
• 年卷期：v.54,no.8(April 28, 2011)
• ISSN：1520-4804

文摘

A series of pegylated distyryl boron dipyrromethenes have been prepared and characterized. Their in vitro photodynamic activities in Tween 80 emulsions have also been investigated against HT29 human colorectal carcinoma cells. The derivative having five triethylene glycol chains (compound 8) exhibits the highest photocytotoxicity with an IC₅₀ as low as 7 nM. It is also localized preferentially in the endoplasmic reticulum of the cells and can induce predominately apoptosis upon illumination.