Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives

Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives

A comprehensive set of 3-phenylcoumarin analogues with polar substituents was synthesised for blocking oestradiol synthesis by 17-β-hydroxysteroid dehydrogenase 1 (HSD1) in the latter part of the sulphatase pathway. Five analogues produced ≥62% HSD1 inhibition at 5 µM and, furthermore, three of them...

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Bibliographic Details
Main Authors: Sanna Niinivehmas, Pekka A. Postila, Sanna Rauhamäki, Elangovan Manivannan, Sami Kortet, Mira Ahinko, Pasi Huuskonen, Niina Nyberg, Pasi Koskimies, Sakari Lätti, Elina Multamäki, Risto O. Juvonen, Hannu Raunio, Markku Pasanen, Juhani Huuskonen, Olli T. Pentikäinen
Format: Article
Language:English
Published: Taylor & Francis Group 2018-01-01
Series:Journal of Enzyme Inhibition and Medicinal Chemistry
Subjects:
3-Phenylcoumarin
17-β-hydroxysteroid dehydrogenase 1 (HSD1)
3-imidazolecoumarin
aromatase
structure-activity relationship (SAR)
Online Access:http://dx.doi.org/10.1080/14756366.2018.1452919

Internet

http://dx.doi.org/10.1080/14756366.2018.1452919

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