Novel Highly Potent and Selective Nonsteroidal Aromatase Inhibitors: Synthesis, Biological Evaluation and Structure−Activity Relationships Investigation

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• 作者：Silvia Gobbi ; Christina Zimmer ; Federica Belluti ; Angela Rampa ; Rolf W. Hartmann ; Maurizio Recanatini ; Alessandra Bisi
• 刊名：Journal of Medicinal Chemistry
• 出版年：2010
• 出版时间：July 22, 2010
• 年：2010
• 卷：53
• 期：14
• 页码：5347-5351
• 全文大小：800K
• 年卷期：v.53,no.14(July 22, 2010)
• ISSN：1520-4804

文摘

In further pursuing our search for potent and selective aromatase inhibitors, a new series of molecules was designed and synthesized, exploring possible structural modifications of a previously identified xanthone scaffold. Among them, highly potent compounds, with inhibitory activity in the low nanomolar range, were found. In particular, substitution of the heterocyclic oxygen atom in the xanthone core by a sulfur atom and/or increase in structure flexibility seemed to be favorable for the interaction with the enzyme.