Synthesis of 2-ethoxycarbonylthieno[2,3-b]quinolines in biomass-derived solvent γ-valerolactone and their biological evaluation against protein tyrosine phosphatase 1B
Author:
Affiliation:
1. School of Pharmaceutical Sciences
2. Jiangnan University
3. Wuxi
4. China
5. State Key Laboratory of Drug Research
6. Shanghai Institute of Materia Medica
7. Chinese Academy of Sciences
8. Shanghai
9. Departamento de Química Orgánica
Abstract
A series of 2-ethoxycarbonylthieno[2,3-b]quinolines were synthesized in the bio-derived “green” solvent γ-valerolactone and evaluated for their inhibitory activities against PTP1B, compound6adisplayed an IC50value of 8.04 ± 0.71 μM with 4.34-fold preference over TCPTP.
Funder
Natural Science Foundation of Jiangsu Province
National Key New Drug Creation and Manufacturing Program, Ministry of Science and Technology
National Natural Science Foundation of China
Publisher
Royal Society of Chemistry (RSC)
Subject
General Chemical Engineering,General Chemistry
Link
http://pubs.rsc.org/en/content/articlepdf/2021/RA/D0RA09247A
Reference49 articles.
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2. Protein Tyrosine Phosphatase-1B Inhibition Disrupts IL13Rα2-Promoted Invasion and Metastasis in Cancer Cells
3. Protein tyrosine phosphatase 1B (PTP1B) inhibitors as potential anti-diabetes agents: patent review (2015-2018)
4. Synthesis of Optically Active 2H-Thiopyrano[2,3-b]quinolines with Three Contiguous Stereocentersviaan Organocatalytic Asymmetric Tandem Michael-Henry Reaction
5. Chemistry of Substituted Quinolines: Thieno[2,3- b ] and Thiopyrano[2,3- b ]quinolines
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