1364440-75-4Relevant academic research and scientific papers
New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series
Stauffer, Frédéric,Furet, Pascal,Floersheimer, Andreas,Lang, Marc
scheme or table, p. 1860 - 1863 (2012/04/17)
Aromatase inhibition is the new standard of care for estrogen receptor positive breast cancer and has also potential for treatment of other diseases such as endometriosis. Simple and readily available 3-pyridyl arylethers and 1-aryl pyrrolo[2,3-c]pyridines recapitulating the key pharmacophore elements of Letrozole (1) are described and their structure-activity relationships are discussed. Potent and ligand efficient leads such as compound 23 (IC 50 = 59 nM on aromatase) have been identified.
