Imidazolylmethylbenzophenones as Highly Potent Aromatase Inhibitors

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• 作者：Silvia Gobbi ; Andrea Cavalli ; Matthias Negri ; Katarzyna E. Schewe ; Federica Belluti ; Lorna Piazzi ; Rolf W. Hartmann ; Maurizio Recanatini ; Alessandra Bisi
• 刊名：Journal of Medicinal Chemistry
• 出版年：2007
• 出版时间：July 26, 2007
• 年：2007
• 卷：50
• 期：15
• 页码：3420 - 3422
• 全文大小：98K
• 年卷期：v.50,no.15(July 26, 2007)
• ISSN：1520-4804

文摘

Suppression of tumor and plasma estrogen levels by inhibition of aromatase is one of the most effective treatments for postmenopausal breast cancer patients. Starting from an easy, syntheticallyaccessible, benzophenone scaffold, a new class of potent aromataseinhibitors was synthesized, endowed with high selectivity with respectto 17-hydroxylase/17,20-lyase (CYP17). Compounds 1b and 1dproved to be among the most potent inhibitors described so far.