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

descriptionPublicationkeyboard_double_arrow_right Article 01 Mar 2006 English Publisher:Elsevier BVJournal:Bioorganic & Medicinal Chemistry Letters, volume 16, pages 1,532-1,536 (issn: 0960-894X,

Authors: Brian E, Fink; Ashvinikumar V, Gavai; John S, Tokarski; Bindu, Goyal; Raj, Misra; Hai-Yun, Xiao; S David, Kimball; +7 Authors

doi: 10.1016/j.bmcl.2005.12.039

pmid: 16386902

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

- Summary
- Subjects
- Related research
  (12)
- Metrics

tips_and_updates
Recommended

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.

Related Organizations

Bristol-Myers Squibb (Germany)
Germany

Keywords

Models, Molecular, 17-Hydroxysteroid Dehydrogenases, Molecular Structure, Androstenedione, Alkaline Phosphatase, Azocines, Structure-Activity Relationship, Humans, Testosterone, Enzyme Inhibitors

12 Research products, page 1 of 2

The (+)- and (−)-gossypols potently inhibit both 3β-hydroxysteroid dehydrogenase and 17β-hydroxysteroid dehydrogenase 3 in human and rat testes
2009IsAmongTopNSimilarDocuments
Disruption of androgen metabolism, regulation and effects : involvement of steroidogenic enzymes
2014IsAmongTopNSimilarDocuments
Inhibition of human and rat 3β-hydroxysteroid dehydrogenase and 17β-hydroxysteroid dehydrogenase 3 activities by perfluoroalkylated substances
2010IsAmongTopNSimilarDocuments
17β-Hydroxysteroid dehydrogenase-3 deficiency: From pregnancy to adolescence
2009IsAmongTopNSimilarDocuments
Development of hormone-dependent prostate cancer models for the evaluation of inhibitors of 17β-hydroxysteroid dehydrogenase Type 3
2009IsAmongTopNSimilarDocuments
Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a series of 4-hydroxyphenyl ketones as potential inhibitors of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3)
2006IsAmongTopNSimilarDocuments
17β-hydroxysteroid dehydrogenase 3 deficiency in a male pseudohermaphrodite
2008IsAmongTopNSimilarDocuments
BindingDB Entry 50017270: Identification of a novel series of tetrahydrodibenzazocines as inhibitors of 17beta-hydroxysteroid dehydrogenase type 3.
2009IsSourceOf
The UV-filter benzophenone-1 inhibits 17β-hydroxysteroid dehydrogenase type 3: Virtual screening as a strategy to identify potential endocrine disrupting chemicals
2010IsAmongTopNSimilarDocuments
Synthesis, biochemical evaluation and rationalisation of the inhibitory activity of a range of 4-hydroxyphenyl ketones as potent and specific inhibitors of the type 3 of 17β-hydroxysteroid dehydrogenase (17β-HSD3)
2008IsAmongTopNSimilarDocuments

chevron_left
1
2
chevron_right

Impact byBIP!

	citations This is an alternative to the "Influence" indicator, which also reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	42
	popularity This indicator reflects the "current" impact/attention (the "hype") of an article in the research community at large, based on the underlying citation network.	Top 10%
	influence This indicator reflects the overall/total impact of an article in the research community at large, based on the underlying citation network (diachronically).	Top 10%
	impulse This indicator reflects the initial momentum of an article directly after its publication, based on the underlying citation network.	Top 10%