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
- dr hab. inż. Sebastian Demkowicz link open in new tab ,
- Kamila Filipiak,
- Maciej Maslyk,
- Jakub Ciepielski,
- Sonia de Pascual-Teresa,
- Sonsoles Martín-Santamaría,
- Beatriz De Pascual-Teresa,
- Ana Ramos
Additional information
- Category
- Publikacja w czasopiśmie
- Type
- artykuł w czasopiśmie wyróżnionym w JCR
- Language
- angielski
- Publication year
- 2013
