Bioorganic & Medicinal Chemistry Letters 2006-03-15

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

Brian E Fink, 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

Index: Bioorg. Med. Chem. Lett. 16(6) , 1532-1536, (2006)

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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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