101596-86-5

Upstream product

• 5720-07-0 4-methoxyphenylboronic acid 
• 144464-64-2 5-oxo-5,6,7,8-tetrahydronaphthalen-2-yl trifluoromethanesulfonate 
• 3470-53-9 6-amino-1-tetralone 
• 66361-67-9 6-bromo-3,4-dihydro-2H-naphthalen-1-one 
• 3470-50-6 6-Hydroxy-1-tetralone 
• 689247-69-6 1,1,2,2,3,3,4,4,5,5,6,6,7,7,8,8,8-heptadecafluoro-octane-1-sulfonic acid 5-oxo-5,6,7,8-tetrahydro-naphthalen-2-yl ester 
• 100-66-3 methoxybenzene 
• 529-34-0 3,4-dihydronaphthalene-1(2H)-one 
• 101594-72-3 6-(4-methoxy-phenyl)-3,4,7,8-tetrahydro-2H-naphthalen-1-one 

Downstream Products

• 101110-09-2 6-(4-hydroxyphenyl)-3,4-dihydronaphthalen-1(2H)-one 
• 110253-10-6 6-(4-methoxyphenyl)-1-naphthol 
• 108976-77-8 6-(4-Methoxy-phenyl)-1,2,3,4-tetrahydro-[1]naphthol 
• 59115-46-7 1-methoxy-6-(4-methoxy-phenyl)-naphthalene 

Relevant academic research and scientific papers

6 - Substituted aryl amino methyl tetralin derivatives or salts thereof, and its preparation and use

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

Discovery of Potent and Selective Agonists of δ Opioid Receptor by Revisiting the "message-Address" Concept

The classic "message-address" concept was proposed to address the binding of endogenous peptides to the opioid receptors and was later successfully applied in the discovery of the first nonpeptide δ opioid receptor (DOR) antagonist naltrindole. By revisiting this concept, and based on the structure of tramadol, we designed a series of novel compounds that act as highly potent and selective agonists of DOR among which (-)-6j showed the highest affinity (Ki = 2.7 nM), best agonistic activity (EC50 = 2.6 nM), and DOR selectivity (more than 1000-fold over the other two subtype opioid receptors). Molecular docking studies suggest that the "message" part of (-)-6j interacts with residue Asp1283.32 and a neighboring water molecule, and the "address" part of (-)-6j packs with hydrophobic residues Leu3007.35, Val2816.55, and Trp2846.58, rendering DOR selectivity. The discovery of novel compound (-)-6j, and the obtained insights into DOR-agonist binding will help us design more potent and selective DOR agonists.

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.

Novel inhibitors of 17β-hydroxysteroid dehydrogenase type 1: Templates for design

The 17β-hydroxysteroid dehydrogenases (17β-HSDs) catalyze the interconversion between the oxidized and reduced forms of androgens and estrogens at the 17 position. The 17β-HSD type 1 enzyme (17β-HSD1) catalyzes the reduction of estrone (E1) to estradiol a

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.

A highly efficient microwave-assisted Suzuki coupling reaction of aryl perfluorooctylsulfonates with boronic acids

A new strategy to improve the efficiency of Suzuki coupling reactions is introduced by combining fast microwave reaction with easy fluorous separation. Aryl perfluorooctylsulfonates derived from the corresponding phenols are coupled with aryl boronic acid

Nonconventional Friedel-Crafts Chemistry. 1. Reaction of α-Tetralone and Anthrone with Arenes under Friedel-Crafts Conditions

α-Tetralone and anthrone were reacted with arenes in the presence of aluminum chloride to give 6-aryl-1-tetralone and 10-arylanthrone, respectively.The mechanism of these reactions are discussed.