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

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

doi:10.1038/srep14195

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

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

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, …

Scientific reports, Vol.5(1), pp.14195-14195

21/09/2015

DOI: https://doi.org/10.1038/srep14195

PMCID: PMC4585680

PMID: 26388336

Abstract

Multidisciplinary Sciences

Science & Technology

Science & Technology - Other Topics

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 triazolothiadiazoles targeting PTP1B and its analogs could be the therapeutic drug-seeds.

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Title: Development of Novel Triazolo-Thiadiazoles from Heterogeneous "Green" Catalysis as Protein Tyrosine Phosphatase 1B Inhibitors
Creators - without role: C. P. Baburajeev - Bangalore University
Chakrabhavi Dhananjaya Mohan - University of Mysore
Hanumappa Ananda - University of Mysore
Shobith Rangappa - Hokkaido University
Julian E. Fuchs - University of Cambridge
Swamy Jagadish - University of Mysore
Kodappully Sivaraman Siveen - Duke-NUS Medical School
Arunachalam Chinnathambi - King Saudi Univ, Coll Sci, Dept Bot & Microbiol, Riyadh 11451, Saudi Arabia
Sulaiman Ali Alharbi - King Saudi Univ, Coll Sci, Dept Bot & Microbiol, Riyadh 11451, Saudi Arabia
M. E. Zayed - King Saudi Univ, Coll Sci, Dept Bot & Microbiol, Riyadh 11451, Saudi Arabia
Jingwen Zhang - Duke-NUS Medical School
Feng Li - National University of Singapore
Gautam Sethi - National University of Singapore
Kesturu S. Girish - University of Mysore
Andreas Bender - University of Cambridge
Basappa - Bangalore University
Kanchugarakoppal S. Rangappa - University of Mysore
Publication Details: Scientific reports, Vol.5(1), pp.14195-14195
Publisher: Springer Nature
Number of pages: 11
Grant note: SR/FT/LS-142/2012 / Vision Group Science and Technology, Department of Science and Technology 45/54/2013-PHA/BMS / ICMR (SRF) European Research Commission; European Commission; European Commission Joint Research Centre Institution of Excellence, University of Mysore 41-257-2012-SR; 39-106/2010 (SR) / University Grants Commission; University Grants Commission, India 01 (2434) /10/ EMR-II / Council of Scientific & Industrial Research; Council of Scientific & Industrial Research (CSIR) - India NUHS Bench-to-Bedside grants Deanship of Scientific Research, College of Science Research Centre, King Saud University, Kingdom of Saudi Arabia
Identifiers: 9949757708331
Academic Unit: King Saud University
Language: English
Resource Type: Journal article