Bioorganic & Medicinal Chemistry Letters 2012-03-01

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

Frédéric Stauffer, Pascal Furet, Andreas Floersheimer, Marc Lang

文献索引：Bioorg. Med. Chem. Lett. 22(5) , 1860-3, (2012)

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摘要

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.Copyright © 2012 Elsevier Ltd. All rights reserved.

相关化合物

  • 2-氯-5-碘甲苯

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