6468-36-6

Upstream product

• 66267-84-3 4-(7-acetoxy-2-oxo-2H-chromen-3-yl)phenyl acetate 
• 156-38-7 4-hydroxyphenylacetate 
• 95-01-2 2,4-Dihydroxybenzaldehyde 
• 104-47-2 p-methoxybenzylnitrile 
• 3173-00-0 7-methoxy-3-(4-methoxyphenyl)-2H-chromen-2-one 
• 673-22-3 2-Hydroxy-4-methoxybenzaldehyde 
• 104-01-8 4-Methoxyphenylacetic acid 
• 66267-82-1 7-hydroxy-3-(4’-methoxyphenyl) coumarin 
• 55453-88-8 sodium 2-(4-hydroxyphenyl)acetate 
• 531-59-9 7-methoxycoumarin 
• 72167-80-7 3-bromo-7-methoxy-2H-chromen-2-one 
• 99-93-4 4-Hydroxyacetophenone 

Downstream Products

• 3173-00-0 7-methoxy-3-(4-methoxyphenyl)-2H-chromen-2-one 
• 252949-47-6 7-methoxymethoxy-3-(4-methoxymethoxyphenyl)-chromen-2-one 
• 1460202-44-1 methyl 3-(2,4-dihydroxyphenyl)-2-(4-hydroxyphenyl)propanoate 
• 1340493-31-3 7-hydroxy-3-(4-hydroxyphenyl)-2H-chroman-2-one 
• 1460202-45-2 3-(2,4-dihydroxyphenyl)-2-(4-hydroxyphenyl)propanoic acid 
• 1460202-47-4 (S)-3-(2,4-dihydroxyphenyl)-2-(4-hydroxyphenyl)propanoic acid (S)-α-methylbenzylamine salt 
• 1460202-50-9 (S)-3-(2,4-dihydroxyphenyl)-2-(4-hydroxyphenyl)propanoic acid (S)-3-aminopiperidine salt 
• 1460202-48-5 (S)-4-(3-hydroxy-2-(4-hydroxyphenyl)propyl)benzene-1,3-diol 
• 531-95-3 equol 

Relevant academic research and scientific papers

Design, Synthesis and Antimicrobial Evaluations of Novel 3,7-Disubstituted 2H-1-Benzopyran-2-ones

In present study, a novel class of 3,7-disubstituted 2H-1-benzopyran-2-one derivatives (3xa-3zc) bearing a basic ether side chain at C-7 and a substituted phenyl ring at C-3 of the coumarin ring is synthesized. These compounds have been evaluated for anti

Synthesis and biological evaluation of 3-arylcoumarin derivatives as potential anti-diabetic agents

A variety of substituted 3-arylcoumarin derivatives were synthesised through microwave radiation heating. The method has characteristics of environmental friendliness, economy, simple separation, and purification process, less by-products and high reaction yield. Those 3-arylcoumarin derivatives were screened for antioxidant, α-glucosidase inhibitory and advanced glycation end-products (AGEs) formation inhibitory. Most compounds exhibited significant antioxidant and AGEs formation inhibitory activities. Anti-diabetic activity studies showed that compounds 11 and 17 were equipotent to the standard drug glibenclamide in vivo. According to the experimental results, the target compound 35 can be used as a lead compound for the development of new anti-diabetic drugs. The whole experiment showed that anti-diabetic activity is prevalent in 3-arylcoumarins, which added a new natural skeleton to the development of anti-diabetic active drugs.

Synthesis and biological evaluation of 3-arylcoumarins as potential anti-Alzheimer's disease agents

Alzheimer's disease, a neurodegenerative illness, has the extremely complex pathogenesis. Accumulating evidence indicates there is a close relationship between several enzymes and Alzheimer's disease. Various substituted 3-arylcoumarin derivatives were synthesised, and their in vitro activity, including cholinesterase inhibitory activity, monoamine oxidase inhibitory activity, and antioxidant activity were investigated. Most of the compounds exhibited high activity; therefore 3-arylcoumarin compounds have the potential as drug candidates for the treatment of Alzheimer's disease.

Coumarin-based emissive hexacatenars: synthesis, 2D and 3D self-assembly and photodimerization

The first examples of unsymmetric coumarin polycatenar liquid crystals consisting of a coumarin central core with 1,2,3-triazole dendritic wings on both sides were synthesized via click reaction. Their properties were investigated using POM, DSC, XRD, SEM

Decarboxylation of α,β-unsaturated aromatic lactones: Synthesis of: E-ortho -hydroxystilbenes from 3-arylcoumarins or isoaurones

A simple and environmentally friendly strategy for the synthesis of E-ortho-hydroxystilbenes has been established. Two kinds of α,β-unsaturated aromatic lactones, i.e. the 3-arylcoumarins and the isoaurones, could both readily undergo a cascade hydrolyzation/decarboxylation reaction in the presence of KOH in ethylene glycol to afford the desired E-ortho-hydroxystilbenes in moderate to high yields.

Molecular Docking-Based Design and Development of a Highly Selective Probe Substrate for UDP-glucuronosyltransferase 1A10

Intestinal and hepatic glucuronidation by the UDP-glucuronosyltransferases (UGTs) greatly affect the bioavailability of phenolic compounds. UGT1A10 catalyzes glucuronidation reactions in the intestine, but not in the liver. Here, our aim was to develop se

Dual functional small molecule fluorescent probes for image-guided estrogen receptor-specific targeting coupled potent antiproliferative potency for breast cancer therapy

A strategy by integrating biological imaging into early stages of the drug discovery process can improve our understanding of drug activity during preclinical and clinical study. In this article, we designed and synthesized coumarin-based nonsteroidal type fluorescence ligands for drug-target binding imaging. Among these synthesized compounds, 3e, 3f and 3h showed potent ER binding affinity and 3e (IC50?=?0.012?μM) exhibited excellent ERα antagonistic activity, its antiproliferative potency in breast cancer MCF-7 cells is equipotent to the approved drug tamoxifen. The fluorescence of compounds 3e and 3f depended on the solvent properties and showed significant changes when mixed with ERα or ERβ in vitro. Furthermore, target molecule 3e could cross the cell membrane, localize and image drug-target interaction in real time without cell washing. Thus, the coumarin-based platform represents a promising new ER-targeted delivery vehicle with potential imaging and therapeutic properties.

PROCESS FOR PRODUCING (S)-EQUOL

The present application relates to an improved process for the preparation of (S)-equol (1). The present application also relates to novel intermediates of formula (7), (7A), (8) and (9) and their use for the synthesis of (5)-equol.

Toward the development of dual-targeted glyceraldehyde-3-phosphate dehydrogenase/ trypanothione reductase inhibitors against trypanosoma brucei and trypanosoma Cruzi

A significant improvement in the treatment of trypanosomiases has been achieved with the recent development of nifurtimox- eflornithine combination therapy (NECT). As an alternative to drug combinations and as a means to overcome most of the antitrypanosomatid drug discovery challenges, a multitarget drug design strategy has been envisaged. To begin testing this hypothesis, we designed and developed a series of quinone-coumarin hybrids against glyceraldehyde-3-phosphate dehydrogenase/trypanothione reductase (GAPDH/TR). These enzymes belong to metabolic pathways that are vital to Trypanosoma brucei and Trypanosoma cruzi, and have thus been considered promising drug targets. The synthesized molecules were characterized for their dual-target antitrypanosomal profile, both in enzyme assays and in in vitro parasite cultures. The merged derivative 2-{[3-(3-dimethylaminopropoxy)- 2-oxo-2H-chromen-7-yl]oxy}anthracene- 1,4-dione (10) showed an IC50 value of 5.4 mm against TbGAPDH and a concomitant Ki value of 2.32 mm against TcTR. Notably, 2-{4-[6-(2-dimethylaminoethoxy)- 2-oxo-2H-chromen-3-yl]phenoxy}anthracene-1,4- dione (compound 6) displayed a remarkable EC50 value for T. brucei parasites (0.026 mm) combined with a very low cytotoxicity toward mammalian L6 cells (7.95 mm). This promising low toxicity of compound 6 might be at least partially due to the fact that it does not interfere with human glutathione reductase.

IMPROVED PROCESS FOR PRODUCING (S)-EQUOL

The present application relates to an improved process for the preparation of (S)- equol (1). The present application also relates to novel intermediates of formula (7), (7A), (8) and (9) and their use for the synthesis of (S)-equol.