Issue 21, 2014

Design and synthesis of paracaseolide A analogues as selective protein tyrosine phosphatase 1B inhibitors

Abstract

A series of structurally related analogues of the natural product paracaseolide A were synthesized and identified as potent PTP1B inhibitors. Among these analogues, compound 10 in particular showed improved PTP1B enzyme inhibitory activity, high selectivity for PTP1B over TC-PTP, and improved cellular effects.

Graphical abstract: Design and synthesis of paracaseolide A analogues as selective protein tyrosine phosphatase 1B inhibitors

Supplementary files

Article information

Article type
Paper
Submitted
27 Jan 2014
Accepted
24 Mar 2014
First published
25 Mar 2014

Org. Biomol. Chem., 2014,12, 3441-3445

Design and synthesis of paracaseolide A analogues as selective protein tyrosine phosphatase 1B inhibitors

J. Yin, C. Tang, L. Gao, W. Ma, J. Li, Y. Li, J. Li and F. Nan, Org. Biomol. Chem., 2014, 12, 3441 DOI: 10.1039/C4OB00214H

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