Search for Potential Non-Steroidal Inhibitors of 17 β-Hydroxysteroid Dehydrogenase (17 β-HSD) in the Treatment of Hormone-Dependent Cancers

Rupinder   K.   Lota; Sachin      Dhanani; Caroline   P.   Owen; Sabbir      Ahmed

doi:10.2174/157018007780077417

Abstract

We report the search for non-steroidal inhibitors of 17β-hydroxysteroid dehydrogenase, in particular, for types 1 and 3. The results show that the synthesised compounds based on the biphenyl backbone were good inhibitors of 17β-HSD1, but were weak inhibitors of 17β-HSD3. The compounds were evaluated against 3β-HSD but showed weak inhibition.

Keywords: 17β-hydroxysteroid dehydrogenase, Type 3, Inhibition, Enzyme inhibition, Biphenyl ketones

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Letters in Drug Design & Discovery

Title: Search for Potential Non-Steroidal Inhibitors of 17 β-Hydroxysteroid Dehydrogenase (17 β-HSD) in the Treatment of Hormone-Dependent Cancers

Volume: 4 Issue: 3

Author(s): Rupinder K. Lota, Sachin Dhanani, Caroline P. Owen and Sabbir Ahmed

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Keywords: 17β-hydroxysteroid dehydrogenase, Type 3, Inhibition, Enzyme inhibition, Biphenyl ketones

Abstract: We report the search for non-steroidal inhibitors of 17β-hydroxysteroid dehydrogenase, in particular, for types 1 and 3. The results show that the synthesised compounds based on the biphenyl backbone were good inhibitors of 17β-HSD1, but were weak inhibitors of 17β-HSD3. The compounds were evaluated against 3β-HSD but showed weak inhibition.

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Lota K. Rupinder, Dhanani Sachin, Owen P. Caroline and Ahmed Sabbir, Search for Potential Non-Steroidal Inhibitors of 17 β-Hydroxysteroid Dehydrogenase (17 β-HSD) in the Treatment of Hormone-Dependent Cancers, Letters in Drug Design & Discovery 2007; 4 (3) . https://dx.doi.org/10.2174/157018007780077417