154548-71-7

Upstream product

• 333-20-0 potassium thioacyanate 
• 104-94-9 4-methoxy-aniline 
• 2632-13-5 2-Bromo-4'-methoxyacetophenone 
• 6037-74-7 2-p-anisidino-1-(4-methoxy-phenyl)-ethanone 

Downstream Products

• 1043600-10-7 4,4'-(2-sulfanyl-1H-imidazol-1,4-diyl)diphenol 
• 367262-73-5 1,4-bis-(4-methoxyphenyl)-1H-imidazole 

Relevant academic research and scientific papers

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

The invention relates to 17beta-hydroxysteroid dehydrogenase type 1 (17betaHSD1) inhibitors, the preparation thereof and the use thereof for the treatment and prophylaxis of hormone-related, especially estrogen-related or androgen-related, diseases.

Design, synthesis and biological evaluation of bis(hydroxyphenyl) azoles as potent and selective non-steroidal inhibitors of 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) for the treatment of estrogen-dependent diseases

The 17β-hydroxysteroid dehydrogenase type 1 (17β-HSD1) catalyses the reduction of the weakly active estrone (E1) into the most potent estrogen, 17β-estradiol (E2). E2 stimulates the growth of hormone-dependent diseases via activation of the estrogen receptors (ERs). 17β-HSD1 is often over-expressed in breast cancer cells. Thus, it is an attractive target for the treatment of mammary tumours. The combination of a ligand- and a structure-based drug design approach led to the identification of bis(hydroxyphenyl) azoles as potential inhibitors of 17β-HSD1. Different azoles and hydroxy substitution patterns were investigated. The compounds were evaluated for activity and selectivity with regard to 17β-HSD2, ERα and ERβ. The most potent compound is 3-[5-(4-hydroxyphenyl)-1,3-oxazol-2-yl]phenol (18, IC50 = 0.31 μM), showing very good selectivity, high cell permeability and medium CaCo-2 permeability.