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

被引：49

作者：

Gobbi, Silvia ^{[1
]}

Zimmer, Christina ^{[2
,3
]}

Belluti, Federica ^{[1
]}

Rampa, Angela ^{[1
]}

Hartmann, Rolf W. ^{[2
,3
]}

Recanatini, Maurizio ^{[1
]}

Bisi, Alessandra ^{[1
]}

机构：

[1] Univ Bologna, Dept Pharmaceut Sci, I-40126 Bologna, Italy

[2] Univ Saarland, D-66041 Saarbrucken, Germany

[3] Helmholtz Inst Pharmaceut Res Saarland, D-66041 Saarbrucken, Germany

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2010年 / 53卷 / 14期

关键词：

ANTITUMOR AGENTS; BREAST-CANCER; XANTHONE DERIVATIVES; PROSTATE-CANCER; IN-VITRO; KETOCONAZOLE; INVIVO; ENZYME; ACIDS; SAR;

D O I：

10.1021/jm100319h

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

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.

引用

页码：5347 / 5351

页数：5

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