Novel and potent 17β-hydroxysteroid dehydrogenase type 1 inhibitors

被引：59

作者：

Lawrence, HR

Vicker, N

Allan, GM

Smith, A

Mahon, MF

Tutill, HJ

Purohit, A

Reed, MJ

Potter, BVL ^{[1
]}

机构：

[1] Univ Bath, Dept Pharm & Pharmacol, Bath BA2 7AY, Avon, England

[2] Univ Bath, Sterix Ltd, Bath BA2 7AY, Avon, England

[3] Univ London Imperial Coll Sci Technol & Med, St Marys Univ, Fac Med, Sterix Ltd, London W2 1NY, England

[4] Univ Bath, Dept Chem, Bath BA2 7AY, Avon, England

来源：

JOURNAL OF MEDICINAL CHEMISTRY | 2005年 / 48卷 / 08期

关键词：

D O I：

10.1021/jm049045r

中图分类号：

R914 [药物化学];

学科分类号：

100701 ;

摘要：

Structure-based drug design using the crystal structure of human 17 beta-hydroxysteroid dehydrogenase type 1 (17 beta-HSD1) led to the discovery of novel, selective, and the most potent inhibitors of 17 beta-HSD1 reported to date. Compounds 1 and 2 contain a side chain with an m-pyridylmethylamide functionality extended from the 16 beta position of a steroid scaffold. A mode of binding is proposed for these inhibitors, and 2 is a steroid-based 17 beta-HSD1 inhibitor with the potential for further development.

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收藏

页码：2759 / 2762

页数：4

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