Abstract
3-Substituted indolin-2-one derivatives had been designed and synthesized as a novel class of protein tyrosine phosphatase 1B (PTP1B) inhibitors. These compounds had been evaluated for their inhibitory activities against PTP1B in vitro with IC50 values in a low micromolar range. Compound 36, the lowest, bore an IC50 value of 3.48 µ M. Preliminary structure-activity relationship was summarized.
Keywords: 3-substituted indolin-2-ones, diabetes, inhibitor, protein tyrosine phosphatase 1B, structure-activity relationship, insulin, receptor, dephosphorylation, leptin, aromaticity group
Letters in Organic Chemistry
Title: Synthesis and Biological Evaluation of Novel Indolin-2-One Derivatives as Protein Tyrosine Phosphatase 1B Inhibitors
Volume: 8 Issue: 7
Author(s): Hou-Ling Dai, Qiang Shen, Jian-Bin Zheng, Jing-Ya Li, Ren Wen and Jia Li
Affiliation:
Keywords: 3-substituted indolin-2-ones, diabetes, inhibitor, protein tyrosine phosphatase 1B, structure-activity relationship, insulin, receptor, dephosphorylation, leptin, aromaticity group
Abstract: 3-Substituted indolin-2-one derivatives had been designed and synthesized as a novel class of protein tyrosine phosphatase 1B (PTP1B) inhibitors. These compounds had been evaluated for their inhibitory activities against PTP1B in vitro with IC50 values in a low micromolar range. Compound 36, the lowest, bore an IC50 value of 3.48 µ M. Preliminary structure-activity relationship was summarized.
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Dai Hou-Ling, Shen Qiang, Zheng Jian-Bin, Li Jing-Ya, Wen Ren and Li Jia, Synthesis and Biological Evaluation of Novel Indolin-2-One Derivatives as Protein Tyrosine Phosphatase 1B Inhibitors, Letters in Organic Chemistry 2011; 8 (7) . https://dx.doi.org/10.2174/157017811796504909
DOI https://dx.doi.org/10.2174/157017811796504909 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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