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Letters in Organic Chemistry

Author(s): Hou-Ling Dai, Qiang Shen, Jian-Bin Zheng, Jing-Ya Li, Ren Wen and Jia Li

DOI: 10.2174/157017811796504909

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Synthesis and Biological Evaluation of Novel Indolin-2-One Derivatives as Protein Tyrosine Phosphatase 1B Inhibitors

Page: [526 - 530] Pages: 5

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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