Selective Toll-like receptor 7 agonists with novel chromeno[3,4-d]imidazol-4(1H)-one and 2-(trifluoromethyl)quinoline/ quinazoline-4-amine scaffolds

Synthesis of imidazolocoumarins by the amide-directed oxidative cyclisation of enol-Ugi derivatives

“…1 TLR7 modulators. 28,29 Scheme 1 Examples of C-H functionalisation via iminium intermediates. [12][13][14][15][16] Scheme 3 Proposed synthesis of imidazolocoumarins.…”

Structural Evolution and Translational Potential for Agonists and Antagonists of Endosomal Toll-like Receptors

“…Dolšak et al further established the importance of a quinazoline core as a TLR7 agonist through ligand-based virtual screening followed by the synthesis of its analogues. The development of the SAR and docking analysis revealed that small flexible alkyl substituents up to 3-carbon length on a four-position amine group or bulky rigid groups are advantageous for showing agonism ( 74 , 75 , 76 ) (Figure ).…”

Conjugate of ibrutinib with a TLR7 agonist suppresses melanoma progression and enhances antitumor immunity

“…Toll-like receptors (TLRs) play an important role in innate and adaptive immunity by recognizing pathogen-associated molecular patterns (PAMPs) present in a variety of viruses and microorganisms [8][9][10][11]. Among these receptors, TLR7, which recognizes single-stranded RNA and synthetic agonists, is expressed by plasmacytoid dendritic cells (pDCs), macrophages and B lymphocytes [12,13]. TLR7 agonists show strong immunostimulatory activity, inducing tumor-specific immune responses and reducing the growth of colon, renal, and breast carcinomas and melanoma [14][15][16].…”