Affiliation: Solvay Pharmaceuticals
Country: The Netherlands
- New inhibitors of 17beta-hydroxysteroid dehydrogenase type 1Josef Messinger
Solvay Pharmaceuticals Research Laboratories, Hannover, Germany
Mol Cell Endocrinol 248:192-8. 2006..Furthermore, the pyrimidinone proved its use in vivo by significantly reducing 17betaHSD1-dependent tumor growth in a new nude mouse model...
- Estrone C15 derivatives--a new class of 17beta-hydroxysteroid dehydrogenase type 1 inhibitorsJosef Messinger
Solvay Pharmaceuticals Research Laboratories, Hans Böckler Allee 20, D 30173 Hannover, Germany
Mol Cell Endocrinol 301:216-24. 2009..In conclusion, estrone C15 derivative compound 21 can be regarded as a promising lead compound for further development as a 17beta-HSD1 inhibitor...
- Human hydroxysteroid (17-beta) dehydrogenase 1 expression enhances estrogen sensitivity of MCF-7 breast cancer cell xenograftsBettina Husen
Solvay Pharmaceuticals Research Laboratories, Hans Böckler Allee 20, 30173 Hannover, Germany
Endocrinology 147:5333-9. 2006..The results evidently show that estrogenic response for E1 is enhanced by the local action of HSD17B1 in vivo, and thus, the enzyme is a potential target for pharmacological inhibition of estrogen action...
- Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1) for the treatment of estrogen-dependent diseaseMartin Frotscher
8 2 Pharmaceutical and Medicinal Chemistry, Saarland University, Saarbrucken, Germany
J Med Chem 51:2158-69. 2008....
- Substituted 6-phenyl-2-naphthols. Potent and selective nonsteroidal inhibitors of 17beta-hydroxysteroid dehydrogenase type 1 (17beta-HSD1): design, synthesis, biological evaluation, and pharmacokineticsSandrine Marchais-Oberwinkler
8 2 Pharmaceutical and Medicinal Chemistry, Saarland University, PO Box 15 11 50, D 66041 Saarbrucken, Germany
J Med Chem 51:4685-98. 2008..The 1-phenyl compound 32 showed a very high inhibitory activity for 17beta-HSD1 (IC50 = 20 nM) and good selectivity (17beta-HSD2 and ERs) and pharmacokinetic properties after peroral application...