Synthesis of 2-ethoxycarbonylthieno[2,3-<i>b</i>]quinolines in biomass-derived solvent γ-valerolactone and their biological evaluation against protein tyrosine phosphatase 1B
link https://doi.org/10.1039/d0ra09247aaccount_box Mu, Xu-Yangaccount_box Wang, Zhi-Jiaaccount_box Feng, Boaccount_box Xu, Leiaccount_box Gao, Li-Xinaccount_box Satheeshkumar, Rajendranaccount_box Li, Jiaaccount_box Zhou, Yu-Boaccount_box Wang, Wen-Long
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A series of 2-ethoxycarbonylthieno[2,3-b]quinolines were synthesized in the bio-derived "green" solvent gamma-valerolactone (GVL) and evaluated for their inhibitory activities against PTP1B, the representative compound 6a displayed an IC50 value of 8.04 +/- 0.71 mu M 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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| Autor | Mu, Xu-Yang Wang, Zhi-Jia Feng, Bo Xu, Lei Gao, Li-Xin Satheeshkumar, Rajendran Li, Jia Zhou, Yu-Bo Wang, Wen-Long |
| Título | Synthesis of 2-ethoxycarbonylthieno[2,3-<i>b</i>]quinolines in biomass-derived solvent γ-valerolactone and their biological evaluation against protein tyrosine phosphatase 1B |
| Revista | Rsc advances |
| ISSN electrónico | 2046-2069 |
| Volumen | 11 |
| Número de publicación | 6 |
| Página inicio | 3216 |
| Página final | 3220 |
| Fecha de publicación | 2021 |
| Resumen | A series of 2-ethoxycarbonylthieno[2,3-b]quinolines were synthesized in the bio-derived "green" solvent gamma-valerolactone (GVL) and evaluated for their inhibitory activities against PTP1B, the representative compound 6a displayed an IC50 value of 8.04 +/- 0.71 mu M 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. |
| Derechos | acceso restringido |
| DOI | 10.1039/d0ra09247a |
| Enlace | |
| Id de publicación en WoS | WOS:000611287900003 |
| Tema ODS | 03 Good Health and Well-being |
| Tema ODS español | 03 Salud y bienestar |
| Tipo de documento | artículo |