In vitro modulatory effects of functionalized pyrimidines and piperidine derivatives on Aryl hydrocarbon receptor (AhR) and glucocorticoid receptor (GR) activities
Jazyk angličtina Země Spojené státy americké Médium print-electronic
Typ dokumentu časopisecké články, práce podpořená grantem
PubMed
28267985
DOI
10.1016/j.bioorg.2017.02.013
PII: S0045-2068(16)30211-5
Knihovny.cz E-zdroje
- Klíčová slova
- Antagonists, Aryl hydrocarbon receptor, Biotransformation, Glucocorticoid receptor, Immunological response, Piperidines, Pyrimidines,
- MeSH
- buňky Hep G2 MeSH
- HeLa buňky MeSH
- lidé MeSH
- molekulární modely MeSH
- objevování léků MeSH
- piperidiny chemie farmakologie MeSH
- pyrimidiny chemie farmakologie MeSH
- receptory aromatických uhlovodíků agonisté antagonisté a inhibitory metabolismus MeSH
- receptory glukokortikoidů agonisté antagonisté a inhibitory metabolismus MeSH
- Check Tag
- lidé MeSH
- Publikační typ
- časopisecké články MeSH
- práce podpořená grantem MeSH
- Názvy látek
- piperidiny MeSH
- pyrimidiny MeSH
- receptory aromatických uhlovodíků MeSH
- receptory glukokortikoidů MeSH
The development of biologically active molecules based on molecular recognition is an attractive and challenging task in medicinal chemistry and the molecules that can activate/deactivate certain receptors are of great medical interest. In this contribution, selected pyrimidine/piperidine derivatives were synthesized and tested for the ability to activate/deactivate Aryl hydrocarbon receptor (AhR) and Glucocorticoid receptor (GR). Tested compounds are shown to activate the receptors but to much lesser extent than positive controls, dioxin and dexamethasone for Ahr and GR, respectively. However, some of them antagonized the positive controls action. Although further in vivo studies are needed to fully characterize the bioactivities of these compounds, the reported in vitro evidences demonstrate that they might be used as the modulators of AhR and GR activities.
Bioinformatics and High Performance Computing Research Group 30107 Murcia Spain
Bioinformatics Centre Biotech Park Sector G Jankipuram Lucknow 226021 Uttar Pradesh India
Department of Cell Biology and Genetics Palacky University Olomouc Czech Republic
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