Literature DB >> 16386902

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

Brian E Fink1, Ashvinikumar V Gavai, John S Tokarski, Bindu Goyal, Raj Misra, Hai-Yun Xiao, S David Kimball, Wen-Ching Han, Derek Norris, Thomas E Spires, Dan You, Marco M Gottardis, Matthew V Lorenzi, Gregory D Vite.   

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.

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Year:  2006        PMID: 16386902     DOI: 10.1016/j.bmcl.2005.12.039

Source DB:  PubMed          Journal:  Bioorg Med Chem Lett        ISSN: 0960-894X            Impact factor:   2.823


  4 in total

Review 1.  Human hydroxysteroid dehydrogenases and pre-receptor regulation: insights into inhibitor design and evaluation.

Authors:  Trevor M Penning
Journal:  J Steroid Biochem Mol Biol       Date:  2011-01-25       Impact factor: 4.292

2.  Substituted Aryl Benzylamines as Potent and Selective Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 3.

Authors:  Nigel Vicker; Helen V Bailey; Joanna M Day; Mary F Mahon; Andrew Smith; Helena J Tutill; Atul Purohit; Barry V L Potter
Journal:  Molecules       Date:  2021-11-26       Impact factor: 4.411

3.  Synthesis and Spectral Characterization of Benzo-[6,7][1,5]diazocino[2,1-a]isoindol-12-(14H)-one Derivatives.

Authors:  Jatinder P Bassin; Bhavani Anagani; Christopher Benham; Madhu Goyal; Maryam Hashemian; Ute Gerhard
Journal:  Molecules       Date:  2016-07-23       Impact factor: 4.411

4.  Rapid and Efficient Microwave-Assisted Friedländer Quinoline Synthesis.

Authors:  Helen V Bailey; Mary F Mahon; Nigel Vicker; Barry V L Potter
Journal:  ChemistryOpen       Date:  2020-11-05       Impact factor: 2.630

  4 in total

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