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设计并合成了一种用于熊果酸衍生物固相合成的双连接子。

Design and synthesis of a dual linker for solid phase synthesis of oleanolic acid derivatives.

机构信息

State Key Laboratory of Bioactive Substances and Functions of Natural Medicines, Institute of Materia Medica, Chinese Academy of Medical Sciences and Peking Union Medical College, 1 Xian Nong Tan Street, Beijing 100050, China.

出版信息

Molecules. 2011 Jun 8;16(6):4748-63. doi: 10.3390/molecules16064748.

Abstract

A hydrophilic amino-terminated poly(ethylene glycol)-type dual linker for solid phase synthesis of oleanolic acid derivatives using trityl chloride resin was designed and synthesized for the first time. Model reactions in both liquid and solid phase were performed to show the feasibility of its selective cleavage at two different sites. The biological assay results indicated that the long and flexible alkyl ether functionality in the linker is less likely to be critical for the binding event. Following the successful solid-phase synthesis of model compounds, the potential of this dual linker in reaction monitoring and target identification is deemed worthy of further study.

摘要

首次设计并合成了一种用于三苯甲基氯树脂固相合成齐墩果酸衍生物的亲水氨基末端聚乙二醇型双连接体。在液相和固相进行了模型反应,以证明其在两个不同部位选择性裂解的可行性。生物测定结果表明,连接体中长而灵活的烷基醚官能团不太可能是结合事件的关键。在模型化合物的固相合成成功后,认为这种双连接体在反应监测和靶标鉴定中的潜力值得进一步研究。

https://cdn.ncbi.nlm.nih.gov/pmc/blobs/b622/6264254/81dffabc2c58/molecules-16-04748-g001.jpg

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