α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases

Authors

  • D. I. Khavrienko
  • O. L. Kobzar
  • M.V. Shevchuk
  • V.D. Romanenko
  • S.M. Kobelev
  • A.D. Averin
  • I.P. Beletskaya
  • A. I. Vovk
  • V.P. Kukhar

DOI:

https://doi.org/10.15407/dopovidi2014.09.109

Keywords:

inhibitory activity, phosphatases, synthesis, α;α-Difluoro-β-ketophosphonates

Abstract

The present study offers a new approach for designing inhibitors of protein tyrosine phosphatases. We have synthesized the cyclam derivatives with α,α-difluoro-β-ketophosphonate fragments covalently attached to tetraazamacrocyclic scaffold, which is known to be of medical interest. The obtained functionalized macrocycles were evaluated as inhibitors of PTP1B, TC-PTP, CD45, and other protein tyrosine phosphatases.

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References

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Published

06.03.2025

How to Cite

Khavrienko, D. I., Kobzar, O. L., Shevchuk, M., Romanenko, V., Kobelev, S., Averin, A., Beletskaya, I., Vovk, A. I., & Kukhar, V. (2025). α,α-Difluoro-β-ketophosphonates on a tetraazamacrocyclic platform: Synthesis and inhibitory activity against protein tyrosine phosphatases . Reports of the National Academy of Sciences of Ukraine, (9), 109–115. https://doi.org/10.15407/dopovidi2014.09.109