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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Publicat a:J Enzyme Inhib Med Chem
Autors principals: Niinivehmas, Sanna, Postila, Pekka A., Rauhamäki, Sanna, Manivannan, Elangovan, Kortet, Sami, Ahinko, Mira, Huuskonen, Pasi, Nyberg, Niina, Koskimies, Pasi, Lätti, Sakari, Multamäki, Elina, Juvonen, Risto O., Raunio, Hannu, Pasanen, Markku, Huuskonen, Juhani, Pentikäinen, Olli T.
Format: Artigo
Idioma:Inglês
Publicat: Taylor & Francis 2018
Matèries:
Research Paper
Accés en línia:https://ncbi.nlm.nih.gov/pmc/articles/PMC6010071/
https://ncbi.nlm.nih.gov/pubmed/29620427
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1080/14756366.2018.1452919
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