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新型系列四氢二苯并氮杂卓作为3型17β-羟基类固醇脱氢酶抑制剂的鉴定

Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3.

作者信息

Fink Brian E, Gavai Ashvinikumar V, Tokarski John S, Goyal Bindu, Misra Raj, Xiao Hai-Yun, Kimball S David, Han Wen-Ching, Norris Derek, Spires Thomas E, You Dan, Gottardis Marco M, Lorenzi Matthew V, Vite Gregory D

机构信息

Department of Oncology Chemistry, Bristol-Myers Squibb Pharmaceutical Research Institute, PO Box 4000, Princeton, NJ 08543-4000, USA.

出版信息

Bioorg Med Chem Lett. 2006 Mar 15;16(6):1532-6. doi: 10.1016/j.bmcl.2005.12.039. Epub 2006 Jan 4.

DOI:10.1016/j.bmcl.2005.12.039
PMID:16386902
Abstract

A novel series of 17beta-hydroxysteroid dehydrogenase type 3 (17beta-HSD3) inhibitors has been identified. These inhibitors, based on a dibenzazocine core, exhibited picomolar to low nanomolar inhibition of 17beta-HSD3 in cell-free enzymatic as well as in cell-based transcriptional reporter assays.

摘要

已鉴定出一系列新型的17β-羟基类固醇脱氢酶3型（17β-HSD3）抑制剂。这些基于二苯并氮杂卓核心的抑制剂，在无细胞酶促以及基于细胞的转录报告基因测定中，对17β-HSD3表现出皮摩尔至低纳摩尔的抑制作用。

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