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New clicked full agonists of the estrogen receptor β

Abstract

A click chemistry approach was used to synthesize a series of 1,4-diaryl-substituted 1,2,3-triazoles designed to behave as estrogen receptor (ER) ligands. We studied their affinities for both receptors α and β, their agonist activities in a cell-based luciferase reporter assay and their effect on the proliferation of the hormone-dependent MCF-7 cell line. We found two compounds (3a and 3c) that behave as selective full agonists for ERβ at a 20 μM concentration, and one of them (3c) showed no proliferative effect on MCF-7 cells.

Authors (8)

  • Photo of dr hab. inż. Sebastian Demkowicz

    Sebastian Demkowicz dr hab. inż.

  • Photo of Kamila Filipiak

    Kamila Filipiak

    • Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
  • Photo of Maciej Maslyk

    Maciej Maslyk

    • Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
  • Photo of Jakub Ciepielski

    Jakub Ciepielski

    • Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
  • Photo of Sonia de Pascual-Teresa

    Sonia de Pascual-Teresa

    • Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
  • Photo of Sonsoles Martín-Santamaría

    Sonsoles Martín-Santamaría

    • Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
  • Photo of Beatriz De Pascual-Teresa

    Beatriz De Pascual-Teresa

    • Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
  • Photo of Ana Ramos

    Ana Ramos

    • Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,

Cite as

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Publication version
Accepted or Published Version
DOI:
Digital Object Identifier (open in new tab) 10.1039/C3RA00122A
License
Copyright (2013 The Royal Society of Chemistry)

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Details

Category:
Articles
Type:
artykuł w czasopiśmie wyróżnionym w JCR
Published in:
RSC Advances no. 3, edition 11, pages 3697 - 3706,
ISSN: 2046-2069
Language:
English
Publication year:
2013
Bibliographic description:
Demkowicz S., Filipiak K., Maslyk M., Ciepielski J., De Pascual-Teresa S., Martín-Santamaría S., De Pascual-Teresa B., Ramos A.: New clicked full agonists of the estrogen receptor β// RSC Advances. -Vol. 3, iss. 11 (2013), s.3697-3706
Verified by:
Gdańsk University of Technology

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