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Patricia Kruchten
Researcher at Saarland University
Publications - 11
Citations - 546
Patricia Kruchten is an academic researcher from Saarland University. The author has contributed to research in topics: Estrogen & Estrogen receptor. The author has an hindex of 11, co-authored 11 publications receiving 530 citations.
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Journal ArticleDOI
Design, Synthesis, Biological Evaluation and Pharmacokinetics of Bis(hydroxyphenyl) substituted Azoles, Thiophenes, Benzenes, and Aza-Benzenes as Potent and Selective Nonsteroidal Inhibitors of 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1)
Emmanuel Bey,Sandrine Marchais-Oberwinkler,Ruth Werth,Matthias Negri,Yaseen A. Al-Soud,Patricia Kruchten,Alexander Oster,Martin Frotscher,Barbara Birk,Rolf W. Hartmann +9 more
TL;DR: The most promising compounds of this study show enhanced IC 50 values in the low nanomolar range, a high selectivity toward 17beta-HSD2, a low binding affinity to ERalpha, a good metabolic stability in rat liver microsomes, and a reasonable pharmacokinetic profile after peroral application.
Journal ArticleDOI
New Insights into the SAR and Binding Modes of Bis(hydroxyphenyl)thiophenes and -benzenes: Influence of Additional Substituents on 17β-Hydroxysteroid Dehydrogenase Type 1 (17β-HSD1) Inhibitory Activity and Selectivity
Emmanuel Bey,Sandrine Marchais-Oberwinkler,Matthias Negri,Patricia Kruchten,Alexander Oster,Tobias Klein,Alessandro Spadaro,Ruth Werth,Martin Frotscher,Barbara Birk,Rolf W. Hartmann +10 more
TL;DR: The fluorine compound 23 exhibits an IC(50) of 8 nM and is the most potent nonsteroidal inhibitor described so far and shows a high selectivity (17beta-HSD2, ERalpha) and excellent pharmacokinetic properties after peroral application to rats.
Journal ArticleDOI
Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseases.
Emmanuel Bey,Sandrine Marchais-Oberwinkler,Patricia Kruchten,Martin Frotscher,Ruth Werth,Alexander Oster,Oztekin Algül,Alexander Neugebauer,Rolf W. Hartmann +8 more
TL;DR: The combination of a ligand- and a structure-based drug design approach led to the identification of bis(hydroxyphenyl) azoles as potential inhibitors of 17beta-HSD1.
Journal ArticleDOI
Development of a biological screening system for the evaluation of highly active and selective 17β-HSD1-inhibitors as potential therapeutic agents
Patricia Kruchten,Ruth Werth,Sandrine Marchais-Oberwinkler,Martin Frotscher,Rolf W. Hartmann +4 more
TL;DR: The development and application of the screening system using the in house library of potential 17beta-HSD1-inhibitors and four potent and selective compounds with a good first pharmacokinetic profile were identified.
Journal ArticleDOI
New drug-like hydroxyphenylnaphthol steroidomimetics as potent and selective 17β-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment of estrogen-dependent diseases.
Sandrine Marchais-Oberwinkler,Marie Wetzel,Erika Ziegler,Patricia Kruchten,Ruth Werth,Claudia Henn,Rolf W. Hartmann,Martin Frotscher +7 more
TL;DR: Inhibition of 17β-HSD1 inhibitors from the hydroxyphenylnaphthol class by introduction of different heteroaromatic rings as well as substituted phenyl groups showed a good membrane permeation and metabolic stability and was orally available in the rat.