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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)
-
Kamila Filipiak
- Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
-
Maciej Maslyk
- Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
-
Jakub Ciepielski
- Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
-
Sonia de Pascual-Teresa
- Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
-
Sonsoles Martín-Santamaría
- Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
-
Beatriz De Pascual-Teresa
- Universidad CEU San Pablo Departamento de Quı ́ mica, Facultad de Farmacia,
-
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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