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Bioorg Chem ; 71: 285-293, 2017 04.
Artigo em Inglês | MEDLINE | ID: mdl-28267985

RESUMO

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.


Assuntos
Piperidinas/química , Piperidinas/farmacologia , Pirimidinas/química , Pirimidinas/farmacologia , Receptores de Hidrocarboneto Arílico/metabolismo , Receptores de Glucocorticoides/metabolismo , Descoberta de Drogas , Células HeLa , Células Hep G2 , Humanos , Modelos Moleculares , Receptores de Hidrocarboneto Arílico/agonistas , Receptores de Hidrocarboneto Arílico/antagonistas & inibidores , Receptores de Glucocorticoides/agonistas , Receptores de Glucocorticoides/antagonistas & inibidores
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