Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17Î²-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study

Article ID	Journal	Published Year	Pages	File Type
5158613	European Journal of Medicinal Chemistry	2017	14 Pages	PDF

Keywords

RBA 17β-Hydroxysteroid dehydrogenase type 1 Dibenzoyl peroxide GnRH Intracrinology N-bromosuccinimide SERM PXR EDD NBS TLC ADME DME DCM 17β-estradiol 3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide MTT NAD(H)NADP(H)Steroidogenic enzymes Estrone absorption, distribution, metabolism, and excretion standard error of the mean Dimethoxyethane Dichloromethane SEM Selective estrogen receptor modulator Enzyme inhibitor nicotinamide adenine dinucleotide phosphate NAD, nicotinamide adenine dinucleotide Gonadotropin-releasing hormone Relative binding affinity Column chromatography TLC, Thin layer chromatography high performance liquid chromatography HPLC Estrogen receptor Pregnane X receptor

Related Topics

Physical Sciences and Engineering Chemistry Organic Chemistry

Preview

Treatment of estrogen-dependent diseases: Design, synthesis and profiling of a selective 17Î²-HSD1 inhibitor with sub-nanomolar IC50 for a proof-of-principle study

Authors

Ahmed S. Abdelsamie, Chris J. van Koppen, Emmanuel Bey, Mohamed Salah, Carsten Börger, Lorenz Siebenbürger, Matthias W. Laschke, Michael D. Menger, Martin Frotscher,