Please use this identifier to cite or link to this item: 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
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