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Multicomponent Functionalization of the Octreotide Peptide Macrocyclic Scaffold
European Journal of Organic Chemistry ( IF 2.5 ) Pub Date : 2022-08-01 , DOI: 10.1002/ejoc.202200687
Aldrin V. Vasco 1 , Leonardo G. Ceballos 2 , Ludger A. Wessjohann 1 , Daniel García Rivera 3
Affiliation  

New octreotide analogs were prepared by replacing the disulfide bond with a functionalized tertiary lactam bridge. The on-resin approach includes an Ugi multicomponent macrocyclization that enables the simultaneous ring closure and incorporation of lipids, fluorophores and functional groups suitable for the subsequent conjugation to cytotoxic moieties.

中文翻译:

奥曲肽大环支架的多组分功能化

通过用功能化的叔内酰胺桥取代二硫键来制备新的奥曲肽类似物。树脂上的方法包括 Ugi 多组分大环化,它能够同时闭环和掺入适合随后与细胞毒性部分缀合的脂质、荧光团和官能团。
更新日期:2022-08-01
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