4.6 Article

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

Journal

ORGANIC & BIOMOLECULAR CHEMISTRY
Volume 12, Issue 21, Pages 3441-3445

Publisher

ROYAL SOC CHEMISTRY
DOI: 10.1039/c4ob00214h

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Funding

  1. National Program on Key Basic Research Project [2012CB524906]
  2. National Natural Science Foundation of China [81125023]
  3. Shanghai Commission of Science and Technology [13DZ2290300]

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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.

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