The discovery of potent small molecule cyclic urea activators of STING.

Eur J Med Chem

Curadev Pharma Pvt. Ltd., B-87, Sector 83, Noida, 201305, Uttar Pradesh, India. Electronic address:

Published: February 2022

STING mediates innate immune responses that are triggered by the presence of cytosolic DNA. Activation of STING to boost antigen recognition is a therapeutic modality that is currently being tested in cancer patients using nucleic-acid based macrocyclic STING ligands. We describe here the discovery of 3,4-dihydroquinazolin-2(1H)-one based 6,6-bicyclic heterocyclic agonists of human STING that activate all known human variants of STING with high potency.

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http://dx.doi.org/10.1016/j.ejmech.2021.114087DOI Listing

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