Development of Novel Triazolo-Thiadiazoles from Heterogeneous “Green” Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors

نویسندگان

  • C. P. Baburajeev
  • Chakrabhavi Dhananjaya Mohan
  • Hanumappa Ananda
  • Shobith Rangappa
  • Julian E. Fuchs
  • Swamy Jagadish
  • Kodappully Sivaraman Siveen
  • Arunachalam Chinnathambi
  • Sulaiman Ali Alharbi
  • M. E. Zayed
  • Jingwen Zhang
  • Feng Li
  • Gautam Sethi
  • Kesturu S. Girish
  • Andreas Bender
  • Basappa
  • Kanchugarakoppal S. Rangappa
چکیده

Condensed-bicyclic triazolo-thiadiazoles were synthesized via an efficient "green" catalyst strategy and identified as effective inhibitors of PTP1B in vitro. The lead compound, 6-(2-benzylphenyl)-3-phenyl-[1,2,4]triazolo[3][1,3,4]thiadiazole (BPTT) was most effective against human hepatoma cells, inhibits cell invasion, and decreases neovasculature in HUVEC and also tumor volume in EAT mouse models. This report describes an experimentally unidentified class of condensed-bicyclic triazolo-thiadiazoles targeting PTP1B and its analogs could be the therapeutic drug-seeds.

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عنوان ژورنال:

دوره 5  شماره 

صفحات  -

تاریخ انتشار 2015