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.
- 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
