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

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 cellul...

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Bibliographic Details
Published in:Organic & biomolecular chemistry 2014-06, Vol.12 (21), p.3441-3445
Main Authors: Yin, Jian-Peng, Tang, Chun-Lan, Gao, Li-Xin, Ma, Wei-Ping, Li, Jing-Ya, Li, Ying, Li, Jia, Nan, Fa-Jun
Format: Article
Language:English
Subjects:
4-Butyrolactone - chemical synthesis
4-Butyrolactone - chemistry
4-Butyrolactone - pharmacology
Drug Design
Enzyme Inhibitors - chemical synthesis
Enzyme Inhibitors - chemistry
Enzyme Inhibitors - pharmacology
Humans
Indicators and Reagents
Insulin - metabolism
Molecular Docking Simulation
Protein Tyrosine Phosphatase, Non-Receptor Type 1 - antagonists & inhibitors
Protein Tyrosine Phosphatase, Non-Receptor Type 1 - metabolism
Receptor, Insulin - metabolism
Signal Transduction - drug effects
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Summary: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.
ISSN:1477-0520
1477-0539
DOI:10.1039/c4ob00214h