ChemMedChem

ChemMedChem · ISSN (e) 1860-7187 · 4 papers in corpus
2022
2-Difluoromethoxy-Substituted Estratriene Sulfamates: Synthesis, Antiproliferative SAR, Antitubulin Activity, and Steroid Sulfatase Inhibition.
doi:10.1002/cmdc.202200408 ·PMID:36109340

2-Difluoromethoxyestratriene derivatives were designed to improve potency and in vivo stability of the drug candidate 2-methoxyestradiol (2ME2). Compound evaluation in vitro against the proliferation of MCF-7 and MDA MB-231 breast cancer ce…

other 2021
N-Phenyl-1,2,3,4-tetrahydroisoquinoline: An Alternative Scaffold for the Design of 17β-Hydroxysteroid Dehydrogenase 1 Inhibitors
doi:10.1002/cmdc.202000762 ·PMID:33151004

17β-Hydroxysteroid dehydrogenases catalyse interconversion at the C17 position between oxidized and reduced forms of steroidal nuclear receptor ligands. The type 1 enzyme, expressed in malignant cells, catalyses reduction of the less-active…

article 2018
Discovery of Vilaprisan (BAY 1002670): A Highly Potent and Selective Progesterone Receptor Modulator Optimized for Gynecologic Therapies
doi:10.1002/cmdc.201800487 ·PMID:30407750

Progesterone plays an important role in the female reproductive system. However, there is also evidence that gynecologic disorders/diseases such as uterine fibroids and endometriosis are progesterone-dependent. Steroidal and non-steroidal s…

other 2011
Bicyclic substituted hydroxyphenylmethanone type inhibitors of 17 β-hydroxysteroid dehydrogenase Type 1 (17 β-HSD1): the role of the bicyclic moiety
doi:10.1002/cmdc.201000457 ·PMID:21337522

An attractive target that has still to be explored for the treatment of estrogen-dependent diseases, such as breast cancer and endometriosis, is the enzyme responsible for the last step in the biosynthesis of estradiol (E2): 17β-hydroxyster…