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

Authors :: Mu XY
Wang ZJ
Feng B
Xu L
Gao LX
Satheeshkumar R
Li J
Zhou YB
Wang WL
Source :: RSC advances [RSC Adv] 2021 Jan 14; Vol. 11 (6), pp. 3216-3220. Date of Electronic Publication: 2021 Jan 14 (Print Publication: 2021).
Publication Year :: 2021
Abstract: 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 <subscript>50</subscript> 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.<br />Competing Interests: The authors have declared no conflict of interest.<br /> (This journal is © The Royal Society of Chemistry.)

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