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In vitro modulatory effects of functionalized pyrimidines and piperidine derivatives on Aryl hydrocarbon receptor (AhR) and glucocorticoid receptor (GR) activities.
Yar, Muhammad; Shahzadi, Lubna; Farooq, Ariba; Jalil Imran, Saima; Cerón-Carrasco, José P; den-Haan, Helena; Kumar, Sanjay; Peña-García, Jorge; Pérez-Sánchez, Horacio; Grycova, Aneta; Dvorak, Zdenek; Vrzal, Radim.
Afiliación
  • Yar M; Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan. Electronic address: drmyar@ciitlahore.edu.pk.
  • Shahzadi L; Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan.
  • Farooq A; Interdisciplinary Research Center in Biomedical Materials, COMSATS Institute of Information Technology, Lahore 54000, Pakistan; Department of Chemistry, The Islamia University of Bahawalpur, Bahawalpur 63100, Pakistan.
  • Jalil Imran S; Department of Cell Biology and Genetics, Palacky University, Olomouc, Czech Republic.
  • Cerón-Carrasco JP; Bioinformatics and High Performance Computing Research Group (BIO-HPC), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain.
  • den-Haan H; Bioinformatics and High Performance Computing Research Group (BIO-HPC), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain.
  • Kumar S; Bioinformatics Centre, Biotech Park, Sector G, Jankipuram, Lucknow 226021, Uttar Pradesh, India.
  • Peña-García J; Bioinformatics and High Performance Computing Research Group (BIO-HPC), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain.
  • Pérez-Sánchez H; Bioinformatics and High Performance Computing Research Group (BIO-HPC), Universidad Católica San Antonio de Murcia (UCAM), 30107 Murcia, Spain.
  • Grycova A; Department of Cell Biology and Genetics, Palacky University, Olomouc, Czech Republic.
  • Dvorak Z; Department of Cell Biology and Genetics, Palacky University, Olomouc, Czech Republic.
  • Vrzal R; Department of Cell Biology and Genetics, Palacky University, Olomouc, Czech Republic. Electronic address: radim.vrzal@email.cz.
Bioorg Chem ; 71: 285-293, 2017 04.
Article en En | MEDLINE | ID: mdl-28267985
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.
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Pirimidinas / Receptores de Glucocorticoides / Receptores de Hidrocarburo de Aril Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2017 Tipo del documento: Article Pais de publicación: Estados Unidos
Texto completo
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Texto completo: 1 Colección: 01-internacional Base de datos: MEDLINE Asunto principal: Piperidinas / Pirimidinas / Receptores de Glucocorticoides / Receptores de Hidrocarburo de Aril Límite: Humans Idioma: En Revista: Bioorg Chem Año: 2017 Tipo del documento: Article Pais de publicación: Estados Unidos