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https://doi.org/10.1038/srep14195
| Title: | Development of novel triazolo-thiadiazoles from heterogeneous "green" catalysis as protein tyrosine phosphatase 1B inhibitors | Authors: | Baburajeev, C.P Dhananjaya Mohan, C Ananda, H Rangappa, S Fuchs, J.E Jagadish, S Sivaraman Siveen, K Chinnathambi, A Ali Alharbi, S Zayed, M.E Zhang, J Li, F Sethi, G Girish, K.S Bender, A Basappa Rangappa, K.S |
Keywords: | 6-(2-benzylphenyl)-3-phenyl-(1,2,4)triazolo(3)(1,3,4)thiadiazole antineoplastic agent benzofuran derivative BIRC5 protein, human caspase 3 chromone derivative cyclin D1 inhibitor of apoptosis protein nicotinamide adenine dinucleotide adenosine diphosphate ribosyltransferase protein bcl 2 protein tyrosine phosphatase 1B PTPN1 protein, human sanggenone C STAT3 protein STAT3 protein, human thiadiazole derivative triazole derivative animal antagonists and inhibitors biosynthesis Carcinoma, Ehrlich Tumor Carcinoma, Hepatocellular cell motion disease model dose response drug effects female G1 phase cell cycle checkpoint Hep-G2 cell line human Liver Neoplasms metabolism molecular model mouse Neovascularization, Pathologic pathology rat Sprague Dawley rat structure activity relation synthesis tumor cell line tumor invasion umbilical vein endothelial cell Animals Antineoplastic Agents Benzofurans Carcinoma, Ehrlich Tumor Carcinoma, Hepatocellular Caspase 3 Cell Line, Tumor Cell Movement Chromones Cyclin D1 Disease Models, Animal Dose-Response Relationship, Drug Female G1 Phase Cell Cycle Checkpoints Hep G2 Cells Human Umbilical Vein Endothelial Cells Humans Inhibitor of Apoptosis Proteins Liver Neoplasms Mice Models, Molecular Neoplasm Invasiveness Neovascularization, Pathologic Poly(ADP-ribose) Polymerases Protein Tyrosine Phosphatase, Non-Receptor Type 1 Proto-Oncogene Proteins c-bcl-2 Rats Rats, Sprague-Dawley STAT3 Transcription Factor Structure-Activity Relationship Thiadiazoles Triazoles |
Issue Date: | 2015 | Publisher: | Nature Publishing Group | Citation: | Baburajeev, C.P, Dhananjaya Mohan, C, Ananda, H, Rangappa, S, Fuchs, J.E, Jagadish, S, Sivaraman Siveen, K, Chinnathambi, A, Ali Alharbi, S, Zayed, M.E, Zhang, J, Li, F, Sethi, G, Girish, K.S, Bender, A, Basappa, Rangappa, K.S (2015). Development of novel triazolo-thiadiazoles from heterogeneous "green" catalysis as protein tyrosine phosphatase 1B inhibitors. Scientific Reports 5 : 14195. ScholarBank@NUS Repository. https://doi.org/10.1038/srep14195 | Abstract: | 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. | Source Title: | Scientific Reports | URI: | https://scholarbank.nus.edu.sg/handle/10635/175483 | ISSN: | 20452322 | DOI: | 10.1038/srep14195 |
| Appears in Collections: | Staff Publications Elements |
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