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

Stauffer F, Frédéric Stauffer, Pascal Furet, Furet P, Andreas Floersheimer, Floersheimer A, Marc Lang, Lang M
Bioorganic & medicinal chemistry letters · 2012 · doi:10.1016/j.bmcl.2012.01.076 · PMID:22335894
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⚙ AI-generated summary by claude@2026-06, 2026-06-13 ⓘ

This study describes new 3-pyridyl arylether and 1-aryl pyrrolo[2,3-c]pyridine compounds as aromatase inhibitors, identifying potent leads like compound 23 (IC(50)=59nM).

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⚙ AI-generated deep summary by claude@2026-06, 2026-06-13 · read from full text ⓘ

The paper reports a medicinal-chemistry study aimed at identifying new aromatase inhibitors from chemical series described as 3-pyridyl arylethers and 1-aryl pyrrolo[2,3-c]pyridines. Using a fluorimetry-based assay measuring inhibition of human aromatase coexpressed with P450 reductase, the authors report multiple enzyme inhibition hits with IC50 values spanning from 1 nM up to 5.03×10^3 nM. A key caveat is that the provided content reflects affinity/enzyme inhibition data for ligand–target pairs without additional details on broader biological validation. The paper does not explicitly discuss endometriosis or adenomyosis; it was included in the corpus via a keyword match in the upstream search index.

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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.
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Report error Found 10 Enz. Inhib. hit(s) with all data for entry = 50034650 Affinity DataIC50: 1nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 59nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 93nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 114nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 229nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 289nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 304nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 523nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 986nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair Affinity DataIC50: 5.03E+3nMAssay Description:Inhibition of human aromatase coexpressed with P450 reductase by fluorimetryMore data for this Ligand-Target Pair

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Condition tags

endometriosis

MeSH descriptors

Aromatase Aromatase Inhibitors Aromatase Inhibitors Breast Neoplasms Pyridines Pyridines Pyrroles Pyrroles Antineoplastic Agents Antineoplastic Agents Antineoplastic Agents Aromatase Aromatase Inhibitors Breast Neoplasms Breast Neoplasms Female Humans Models, Molecular Pyridines Pyrroles

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europepmc
last seen: 2026-07-31T06:09:14.520117+00:00
pubmed
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