Bioorganic & medicinal chemistry letters

3-Aminoxypropionate-based linker system for cyclization activation in prodrug design

Y Ge, X Wu, D Zhang, L Hu

文献索引：Ge, Yiyu; Wu, Xinghua; Zhang, Dazhi; Hu, Longqin Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 941 - 944

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被引用次数: 7

摘要

A novel linker system based on 3-aminoxypropionate was designed and evaluated for drug release using proteolysis as an activation trigger followed by intramolecular cyclization. The hydroxylamine moiety present in the linker system enabled faster release of the parent drug from the linker–drug conjugate at lower pH as compared to an aliphatic amine moiety. Introduction of two methyl groups strategically at the α position to the carboxylate in the ...