Synthesis of 2-ethoxycarbonylthieno[2,3-b]quinolines in biomass-derived solvent γ-valerolactone and their biological evaluation against protein tyrosine phosphatase 1B

A series of 2-ethoxycarbonylthieno[2,3-b]quinolines were synthesized in the bio-derived “green” solvent γ-valerolactone (GVL) and evaluated for their inhibitory activities against PTP1B, the representative compound 6a displayed an IC(50) value of 8.04 ± 0.71 μM with 4.34-fold preference over TCPTP....

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Detalles Bibliográficos
Autores principales: Mu, Xu-Yang, Wang, Zhi-Jia, Feng, Bo, Xu, Lei, Gao, Li-Xin, Satheeshkumar, Rajendran, Li, Jia, Zhou, Yu-Bo, Wang, Wen-Long
Formato: Online Artículo Texto
Lenguaje:English
Publicado: The Royal Society of Chemistry 2021
Materias:
Chemistry
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC8694002/
https://www.ncbi.nlm.nih.gov/pubmed/35424294
http://dx.doi.org/10.1039/d0ra09247a
Descripción
Sumario:A series of 2-ethoxycarbonylthieno[2,3-b]quinolines were synthesized in the bio-derived “green” solvent γ-valerolactone (GVL) and evaluated for their inhibitory activities against PTP1B, the representative compound 6a displayed an IC(50) value of 8.04 ± 0.71 μM with 4.34-fold preference over TCPTP. These results provided novel lead compounds for the design of inhibitors of PTP1B as well as other PTPs.

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