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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...
| Autores principales: | , , , , , , , , , , , , , , , , |
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| Formato: | Online Artículo Texto |
| Lenguaje: | English |
| Publicado: |
Nature Publishing Group
2015
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| Materias: | |
| 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 |
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| author | 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. |
| author_facet | 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. |
| author_sort | Baburajeev, C. P. |
| collection | PubMed |
| description | 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. |
| format | Online Article Text |
| id | pubmed-4585680 |
| institution | National Center for Biotechnology Information |
| language | English |
| publishDate | 2015 |
| publisher | Nature Publishing Group |
| record_format | MEDLINE/PubMed |
| spelling | pubmed-45856802015-09-29 Development of Novel Triazolo-Thiadiazoles from Heterogeneous “Green” Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors 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. Sci Rep Article 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. Nature Publishing Group 2015-09-21 /pmc/articles/PMC4585680/ /pubmed/26388336 http://dx.doi.org/10.1038/srep14195 Text en Copyright © 2015, Macmillan Publishers Limited http://creativecommons.org/licenses/by/4.0/ This work is licensed under a Creative Commons Attribution 4.0 International License. The images or other third party material in this article are included in the article’s Creative Commons license, unless indicated otherwise in the credit line; if the material is not included under the Creative Commons license, users will need to obtain permission from the license holder to reproduce the material. To view a copy of this license, visit http://creativecommons.org/licenses/by/4.0/ |
| spellingShingle | Article 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. Development of Novel Triazolo-Thiadiazoles from Heterogeneous “Green” Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors |
| title | Development of Novel Triazolo-Thiadiazoles from Heterogeneous “Green” Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors |
| title_full | Development of Novel Triazolo-Thiadiazoles from Heterogeneous “Green” Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors |
| title_fullStr | Development of Novel Triazolo-Thiadiazoles from Heterogeneous “Green” Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors |
| title_full_unstemmed | Development of Novel Triazolo-Thiadiazoles from Heterogeneous “Green” Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors |
| title_short | Development of Novel Triazolo-Thiadiazoles from Heterogeneous “Green” Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors |
| title_sort | development of novel triazolo-thiadiazoles from heterogeneous “green” catalysis as protein tyrosine phosphatase 1b inhibitors |
| topic | Article |
| url | https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4585680/ https://www.ncbi.nlm.nih.gov/pubmed/26388336 http://dx.doi.org/10.1038/srep14195 |
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