Design, synthesis and biological evaluation of novel arylidine-malononitrile derivatives as non-carboxylic inhibitors of protein tyrosine phosphatase 1B

In this study, we describe the design, synthesis, biological evaluation and molecular modelling studies of novel non-carboxylic arylidine malononitrile-based molecules as Protein Tyrosine Phosphatase 1B (PTP1B) inhibitors. The synthesized derivatives were evaluated in vitro for glucose reuptake usin...

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Bibliographic Details
Published in:Medicinal chemistry research 2013-11, Vol.22 (11), p.5344-5348
Main Authors: Deora, Girdhar Singh, Karthikeyan, Chandrabose, Moorthy, N. S. Hari Narayana, Rathore, Vandana, Rawat, Arun K., Tamrakar, Akhilesh K., Srivastava, A. K., Trivedi, Piyush
Format: Article
Language:English
Subjects:
Biochemistry
Biomedical and Life Sciences
Biomedicine
Cell Biology
Original Research
Pharmacology/Toxicology
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Summary:In this study, we describe the design, synthesis, biological evaluation and molecular modelling studies of novel non-carboxylic arylidine malononitrile-based molecules as Protein Tyrosine Phosphatase 1B (PTP1B) inhibitors. The synthesized derivatives were evaluated in vitro for glucose reuptake using L6 muscle cell lines and enzymatic assay against PTP1B. The biological activity results showed that the 2-methoxy substituted ( 14b ) compound exhibited significant activity in both the assays. The unsubstituted compound ( 14a ) also possessed comparable activity on glucose reuptake in L6 muscle cell lines and better inhibitory activity on PTP1B enzyme assays. Docking analysis was performed on the most potent compound of the series to understand the nature of interactions governing the binding of the designed molecule with the PTP1B enzyme.
ISSN:1054-2523
1554-8120
DOI:10.1007/s00044-013-0528-1