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

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

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Bibliographic Details
Published in:Bioorganic & medicinal chemistry letters 2006-03, Vol.16 (6), p.1532-1536
Main Authors: 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.
Format: Article
Language:English
Subjects:
17β-HSD3
Androstenedione
Antineoplastic agents
Biological and medical sciences
General aspects
Hydroxysteroid dehydrogenase
Medical sciences
Pharmacology. Drug treatments
Prostate cancer
Tetrahydrodibenzazocine
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Summary:A novel series of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitors has been identified. These inhibitors, based on a dibenzazocine core, exhibited picomolar to low nanomolar inhibition of 17β-HSD3 in cell-free enzymatic as well as in cell-based transcriptional reporter assays. A novel series of 17β-hydroxysteroid dehydrogenase type 3 (17β-HSD3) inhibitors has been identified. These inhibitors, based on a dibenzazocine core, exhibited picomolar to low nanomolar inhibition of 17β-HSD3 in cell-free enzymatic as well as in cell-based transcriptional reporter assays.
ISSN:0960-894X
1464-3405
DOI:10.1016/j.bmcl.2005.12.039