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

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- ]quinoline synthesized a Povarov-Doebner MCR. HSKB142 is non-cytotoxic towards immune cells and suppresses type-1 i...

Full description

Saved in:
Bibliographic Details
Published in:Chemical communications (Cambridge, England) England), 2024-10, Vol.60 (83), p.11932-11935
Main Authors: Owusu, Kofi B, Samal, Jyotrimayee, Hernandez, Delmis E, Sintim, Herman O
Format: Article
Language:English
Subjects:
Administration, Oral
Bioavailability
Chemical synthesis
Humans
Immune system
Interferon Type I - metabolism
Membrane Proteins - antagonists & inhibitors
Membrane Proteins - metabolism
Molecular Structure
Pyrazoles - chemical synthesis
Pyrazoles - chemistry
Pyrazoles - pharmacology
Quinoline
Quinolines - chemistry
Quinolines - pharmacology
THP-1 Cells
Citations: Items that this one cites
Online Access:Get full text
Tags: Add Tag
No Tags, Be the first to tag this record!
Description
Summary: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- ]quinoline synthesized 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.
ISSN:1359-7345
1364-548X
1364-548X
DOI:10.1039/d4cc03228d