101596-86-5Relevant articles and documents
6 - Substituted aryl amino methyl tetralin derivatives or salts thereof, and its preparation and use
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Paragraph 0037; 0038; 0039; 0088; 0089; 0090; 0091; 0092, (2018/04/02)
The invention provides a 6-substituted aryl amino methyl tetrahydronaphthalene derivative or salt thereof and a preparation method and application of the 6-substituted aryl amino methyl tetrahydronaphthalene derivative, belongs to the pharmaceutical field
17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES
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Page/Page column 20-21, (2010/08/18)
The invention relates to the use of non-steroidal 17beta-hydroxysteroid dehydrogenase type 1 inhibitors for the treatment and prophylaxis of hormone-dependent, particularly estrogen-dependent, diseases.The invention further relates to suitable inhibitors and to a method for the production thereof.
Design, synthesis, and biological evaluation of (hydroxyphenyl)naphthalene and -quinoline derivatives: Potent and selective nonsteroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases
Frotscher, Martin,Ziegler, Erika,Marchais-Oberwinkler, Sandrine,Kruchten, Patricia,Neugebauer, Alexander,Fetzer, Ludivine,Scherer, Christiane,Müller-Vieira, Ursula,Messinger, Josef,Thole, Hubert,Hartmann, Rolf W.
, p. 2158 - 2169 (2008/12/20)
Human 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyzes the reduction of the weak estrogen estrone (E1) to the highly potent estradiol (E2). This reaction takes place in the target cell where the estrogenic effect is exerted via the estrogen receptor (ER). Estrogens, especially E2, are known to stimulate the proliferation of hormone-dependent diseases. 17β-HSD1 is overexpressed in many breast tumors. Thus, it is an attractive target for the treatment of these diseases. Ligand- and structure-based drug design led to the discovery of novel, selective, and potent inhibitors of 17β-HSD1. Phenyl-substituted bicyclic moieties were synthesized as mimics of the steroidal substrate. Computational methods were used to obtain insight into their interactions with the protein. Compound 5 turned out to be a highly potent inhibitor of 17β-HSD1 showing good selectivity (17β-HSD2, ERα and β), medium cell permeation, reasonable metabolic stability (rat hepatic microsomes), and little inhibition of hepatic CYP enzymes.