Blocking oestradiol synthesis pathways with potent and selective coumarin derivatives

• Main Authors: Sanna Niinivehmas (Author), Pekka A. Postila (Author), Sanna Rauhamäki (Author), Elangovan Manivannan (Author), Sami Kortet (Author), Mira Ahinko (Author), Pasi Huuskonen (Author), Niina Nyberg (Author), Pasi Koskimies (Author), Sakari Lätti (Author), Elina Multamäki (Author), Risto O. Juvonen (Author), Hannu Raunio (Author), Markku Pasanen (Author), Juhani Huuskonen (Author), Olli T. Pentikäinen (Author)
• Format: Book
• Published: Taylor & Francis Group, 2018-01-01T00:00:00Z.
• Subjects: article
• Online Access: Connect to this object online.

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...