Phosphonate monoesters on a thiacalix[4]arene framework as potential inhibitors of protein tyrosine phosphatase 1B

Viacheslav V Trush; Sergiy G Kharchenko; Vsevolod Yu Tanchuk; Vitaly I Kalchenko; Andriy I Vovk

doi:10.1039/c5ob01247c

Phosphonate monoesters on a thiacalix[4]arene framework as potential inhibitors of protein tyrosine phosphatase 1B

Org Biomol Chem. 2015 Sep 7;13(33):8803-6. doi: 10.1039/c5ob01247c. Epub 2015 Jul 24.

Authors

Viacheslav V Trush¹, Sergiy G Kharchenko, Vsevolod Yu Tanchuk, Vitaly I Kalchenko, Andriy I Vovk

Affiliation

¹ Department of Bioorganic Mechanisms, Institute of Bioorganic Chemistry and Petrochemistry of National Academy of Sciences of Ukraine, Kyiv, Ukraine. [email protected].

PMID: 26205135
DOI: 10.1039/c5ob01247c

Abstract

Monoester derivatives of thiacalix[4]arene tetrakis(methylphosphonic) acid were found to be capable of inhibiting protein tyrosine phosphatase 1B. In addition, these compounds can strongly bind to human serum albumin.

MeSH terms

Calixarenes / chemistry
Calixarenes / pharmacology*
Catalytic Domain
Enzyme Inhibitors / chemistry
Enzyme Inhibitors / pharmacology*
Esters / chemistry
Esters / pharmacology*
Humans
Inhibitory Concentration 50
Kinetics
Models, Molecular
Organophosphonates / chemistry
Organophosphonates / pharmacology*
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / antagonists & inhibitors*
Protein Tyrosine Phosphatase, Non-Receptor Type 1 / metabolism
Serum Albumin / metabolism
Temperature

Substances

Enzyme Inhibitors
Esters
Organophosphonates
Serum Albumin
Calixarenes
Protein Tyrosine Phosphatase, Non-Receptor Type 1