110253-10-6

Upstream product

• 101596-86-5 6-(4-methoxyphenyl)-3,4-dihydronaphthalen-1(2H)-one 
• 1078-19-9 6-methoxy-3,4-dihydro-1(2H)-naphthalenone 
• 144464-64-2 5-oxo-5,6,7,8-tetrahydronaphthalen-2-yl trifluoromethanesulfonate 
• 3470-50-6 6-Hydroxy-1-tetralone 
• 1268826-55-6 5-hydroxy-2-naphthyl trifluoromethanesulfonate 
• 5720-07-0 4-methoxyphenylboronic acid 
• 1268826-54-5 6-bromo-5-oxo-5,6,7,8-tetrahydro-2-naphthyl trifluoromethanesulfonate 
• 101594-72-3 6-(4-methoxy-phenyl)-3,4,7,8-tetrahydro-2H-naphthalen-1-one 

Downstream Products

• 59115-46-7 1-methoxy-6-(4-methoxy-phenyl)-naphthalene 

Relevant academic research and scientific papers

17β-HSD2 inhibitors for the treatment of osteoporosis: Identification of a promising scaffold

17β-Hydroxysteroid dehydrogenase type 2 (17β-HSD2) catalyses the conversion of active 17β-hydroxysteroids into the less active 17-ketosteroids thereby controlling the availability of biologically active estrogens (E2) and androgens (T) in the tissues. The skeletal disease osteoporosis occurs mainly in post-menopausal women and in elderly men when the levels of estrogens and androgens, respectively, decrease. Since 17β-HSD2 is present in osteoblasts, inhibition of this enzyme may provide a new and promising approach to prevent the onset of osteoporosis, keeping a certain level in estrogens and androgens in bone cells of ageing people. Hydroxynaphthyl, hydroxyphenyl and hydroxymethylphenyl-substituted moieties were synthesised as mimetics of the steroidal substrate. Compound 8 has been identified as promising scaffold for 17β-HSD2 inhibitors displaying high activity and good selectivity toward 17β-HSD1, ERα and ERβ.

17BETA-HYDROXYSTEROID DEHYDROGENASE TYPE 1 INHIBITORS FOR THE TREATMENT OF HORMONE-RELATED DISEASES

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

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.