1064680-99-4

Upstream product

• 135-19-3 β-naphthol 
• 127399-79-5 2-(benzyloxy)-1,6-dibromonaphthalene 
• 66996-59-6 1,6-dibromo-2-methoxynaphthalene 
• 16239-18-2 1,6-dibromo-2-naphthol 
• 5111-65-9 2-Bromo-6-methoxynaphthalene 
• 1365958-40-2 2-(benzyloxy)-6-(3-(benzyloxy)phenyl)-1-bromonaphthalene 
• 1365958-67-3 N-(3-(2-(benzyloxy)-6-(3-(benzyloxy)phenyl)naphthalen-1-yl)phenyl)-3-nitrobenzenesulfonamide 
• 1365958-43-5 3-(2-(benzyloxy)-6-(3-(benzyloxy)phenyl)naphthalen-1-yl)aniline 
• 1064680-92-7 1-(3-aminophenyl)-6-(3-hydroxyphenyl)naphthalen-2-ol 
• 121-51-7 3-nitrobenzenesulphonyl chloride 
• 1064681-42-0 3-(2-methoxy-6-(3-methoxyphenyl)naphthalen-1-yl)aniline 
• 1041115-67-6 1-bromo-2-methoxy-6-(3-methoxyphenyl)naphthalene 

Relevant academic research and scientific papers

Lead optimization of 17β-HSD1 inhibitors of the (hydroxyphenyl) naphthol sulfonamide type for the treatment of endometriosis

The reduction of estrone to estradiol, the most potent estrogen in human, is catalyzed by 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1). A promising approach for the treatment of estrogen-dependent diseases is the reduction of intracellular estradiol formation by inhibition of 17β-HSD1. For the species-specific optimization of the (hydroxyphenyl)naphthols, a combinatorial approach was applied and enhanced by a focused synthesis that resulted in the aromatic-substituted (hydroxyphenyl)naphthol sulfonamides. Rigidification of 12 led to the 4-indolylsulfonamide 30, which is a highly active and selective human 17β-HSD1 inhibitor, as well as a highly potent and selective inhibitor of 17β-HSD1 from Callithrix jacchus. It shows no affinity to the estrogen receptors I?± and β and good intracellular activity (T47D). Thus, compound 30 shows good properties for further ADMET studies and might be a candidate for the in vivo proof of concept in C. jacchus.

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.