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Modular Synthesis of Cell-Permeating 2-Ketoglutarate Esters.
- Source :
-
Organic Letters . May2015, Vol. 17 Issue 10, p2326-2329. 4p. - Publication Year :
- 2015
-
Abstract
- Cell-permeating esters of 2-ketoglutarate (2-KG) have been synthesized through a convergent sequence from two modules in two and three steps, respectively. This route provides access to a full series of mono- and disubstituted 2-KG esters, enabling us to define the effect of regioisomeric masking on metabolite release and antihypoxic activity in cell-based assays. In addition to providing insight into the biological activity of cell permeable 2-KG esters, the straightforward and modular nature of this synthetic route may prove useful for the development of next-generation 2-KG analogues for diagnostic and therapeutic applications. [ABSTRACT FROM AUTHOR]
- Subjects :
- *CHEMICAL synthesis
*ESTERS analysis
*METABOLITE analysis
*ISOMERS
*BIOLOGICAL assay
Subjects
Details
- Language :
- English
- ISSN :
- 15237060
- Volume :
- 17
- Issue :
- 10
- Database :
- Academic Search Index
- Journal :
- Organic Letters
- Publication Type :
- Academic Journal
- Accession number :
- 102774786
- Full Text :
- https://doi.org/10.1021/acs.orglett.5b00737