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

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, i...

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Detalles Bibliográficos
Autores principales: Baburajeev, C. P., Dhananjaya Mohan, Chakrabhavi, Ananda, Hanumappa, Rangappa, Shobith, Fuchs, Julian E., Jagadish, Swamy, Sivaraman Siveen, Kodappully, Chinnathambi, Arunachalam, Ali Alharbi, Sulaiman, Zayed, M. E., Zhang, Jingwen, Li, Feng, Sethi, Gautam, Girish, Kesturu S., Bender, Andreas, Basappa, Rangappa, Kanchugarakoppal S.
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Nature Publishing Group 2015
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4585680/
https://www.ncbi.nlm.nih.gov/pubmed/26388336
http://dx.doi.org/10.1038/srep14195
Descripción
Sumario: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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