Issue 83, 2024

Orally bioavailable STING antagonist synthesized via multi-component Povarov–Doebner type reaction

Abstract

Aberrant activation of the cGAS-STING signaling results in innate immune response induction. Herein, we report HSKB142, an orally bioavailable compound containing the 3H-pyrazolo [4,3-f]quinoline synthesized via a Povarov–Doebner MCR. HSKB142 is non-cytotoxic towards immune cells and suppresses type-1 interferon expression in human THP-1 monocytes upon treatment with 2′3′-cGAMP.

Graphical abstract: Orally bioavailable STING antagonist synthesized via multi-component Povarov–Doebner type reaction

Supplementary files

Article information

Article type
Communication
Submitted
02 Jul 2024
Accepted
19 Sep 2024
First published
20 Sep 2024
This article is Open Access
Creative Commons BY license

Chem. Commun., 2024,60, 11932-11935

Orally bioavailable STING antagonist synthesized via multi-component Povarov–Doebner type reaction

K. B. Owusu, J. Samal, D. E. Hernandez and H. O. Sintim, Chem. Commun., 2024, 60, 11932 DOI: 10.1039/D4CC03228D

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