New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.

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Stauffer F, Furet P, Floersheimer A, Lang M

New aromatase inhibitors from the 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine series.

Bioorg Med Chem Lett. 2012 Mar 1;22(5):1860-3. doi: 10.1016/j.bmcl.2012.01.076. Epub 2012 Jan 28.

PubMed ID

22335894 [ View in PubMed

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Abstract

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)=59nM on aromatase) have been identified.

DrugBank Data that Cites this Article

Binding Properties

Drug	Target	Property	Measurement	pH	Temperature (°C)
Letrozole	Cytochrome P450 19A1	IC 50 (nM)	1	N/A	N/A	Details