1.
Bioorg Med Chem
; 22(1): 126-34, 2014 Jan 01.
Artigo
em Inglês
| MEDLINE
| ID: mdl-24345481
RESUMO
Fluorinated isoflavanones and bifunctionalized isoflavanones were synthesized through a one-step gold(I)-catalyzed annulation reaction. These compounds were evaluated for their in vitro inhibitory activities against aromatase in a fluorescence-based enzymatic assay. Selected compounds were tested for their anti-proliferative effects on human breast cancer cell line MCF-7. Compounds 6-methoxy-3-(pyridin-3-yl)chroman-4-one (3c) and 6-fluoro-3-(pyridin-3-yl)chroman-4-one (3e) were identified as the most potent aromatase inhibitors with IC50 values of 2.5 µM and 0.8 µM. Therefore, these compounds have great potential for the development of pharmaceutical agents against breast cancer.