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Selective Toll-like receptor 7 agonists with novel chromeno[3,4-d]imidazol-4(1H)-one and 2-(trifluoromethyl)quinoline/ quinazoline-4-amine scaffoldsDolšak, Ana, farmacevtka, 1993- ...Toll-like receptors (TLRs) are promising targets for treatment of viral infections, autoimmune diseases, and cancers. Here, two new series of selective small-molecule TLR7 agonists with novel ... scaffolds and good selectivity over TLR8 are described, some with potencies in the low micromolar range. 8-Hydroxy-1-isobutylchromeno[3,4-d]imidazol-4(1H)-one (26) from the first series was designed and synthesized on the basis of previously described TLR7 antagonist 2, and is shown to be a selective TLR7 agonist (EC50, 1.8[micro]M). The second series was based on 2-(trifluoromethyl)quinolin-4-amine and 2-(trifluoromethyl)quinazolin-4-amine scaffolds, which were defined according to our in-house ligand-based virtual screening protocol. Further synthesis of a focused library of analogs, biological evaluation, and docking studies provided systematic exploration of the structure-activity relationships, which indicate that a secondary or tertiary amine with smaller flexible alkyl substituents up to three carbon atoms in length, or bulkier rigid aliphatic rings is required at position 4 on 2-(trifluoromethyl)quinoline/quinazoline scaffold for potent TLR7 agonist activity. The influence of selected TLR7 agonists on cytokine production is also reported showing that N-cyclopropyl-2-(trifluoromethyl)quinazolin-4-amine (46) is able to induce increased levels of IL-6 and IL-8. These data demonstrate successful in-silico definition of novel TLR7 versus TLR8-selective compounds as promising chemical probes for further development of potent small-molecule immunomodulators.Source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 179, Oct. 2019, str. 109-122)Type of material - article, component part ; adult, seriousPublish date - 2019Language - englishCOBISS.SI-ID - 34389209
Link(s):
https://www.sciencedirect.com/science/article/pii/S0223523419305586Dostop preko računalnikov UL
source: European journal of medicinal chemistry. - ISSN 0223-5234 (Vol. 179, Oct. 2019, str. 109-122)
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JCR | SNIP | JCR | SNIP | JCR | SNIP | JCR | SNIP |
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DRS, in which the journal is indexed
Database name | Field | Year |
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Links to authors' personal bibliographies | Links to information on researchers in the SICRIS system |
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Dolšak, Ana, farmacevtka, 1993- | 50400 |
Švajger, Urban | 26198 |
Lešnik, Samo | 37452 |
Konc, Janez | 25435 |
Gobec, Stanislav, 1970- | 15284 |
Sova, Matej, 1979- | 25490 |
Source: Personal bibliographies
and: SICRIS
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