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A General Strategy for the Preparation of Thalidomide-Conjugate Linkers
Synlett ( IF 2 ) Pub Date : 2017-08-23 , DOI: 10.1055/s-0036-1588539
James Papatzimas 1 , Evgueni Gorobets 1 , Duncan Brownsey 1 , Ranjan Maity 2 , Nizar Bahlis 2 , Darren Derksen 1
Affiliation  

The synthesis of small-molecule linkers for installation of thalidomide-based conjugates is described. Linker properties have been recognized as vital to conjugate success in drug discovery and delivery systems. These small-molecule tethers act as linkages between molecules, can also aid in cell permeability, and act as solubilizing agents. This work shows our progress in synthesizing conjugates with a variety of linker characteristics. The adaptability and manipulation of these and other linkers holds potential in improving synthetic control of chemical connectivities toward therapeutic development.

中文翻译:

沙利度胺-共轭接头制备的一般策略

描述了用于安装基于沙利度胺的偶联物的小分子接头的合成。接头特性已被认为是药物发现和递送系统中偶联物成功的关键。这些小分子系链充当分子之间的连接,还可以帮助细胞通透性,并充当增溶剂。这项工作展示了我们在合成具有各种接头特征的偶联物方面取得的进展。这些和其他连接器的适应性和操作在改善化学连接的合成控制以促进治疗发展方面具有潜力。
更新日期:2017-08-23
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