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Upstream product

• 1197-09-7 1-(3,4-dihydroxyphenyl)ethan-1-one 
• 139-85-5 3,4-dihydroxybenzaldehyde 
• 120-14-9 3,4-dimethoxy-benzaldehyde 
• 6515-06-6 3,4-bis-methoxymethoxy-benzaldehyde 
• 1131-62-0 1-(3,4-dimethoxyphenyl)ethanone 
• 130768-85-3 (E)-1-(3,4-dimethoxyphenyl)-3-(3,4-dimethoxyphenyl)prop-2-en-1-one 
• 7355-34-2 1,3‐bis(3,4‐dimethoxyphenyl)prop‐2‐en‐1‐one 

Relevant academic research and scientific papers

Analogues of xanthones——Chalcones and bis-chalcones as α-glucosidase inhibitors and anti-diabetes candidates

Two series of compounds (chalcones and bis-chalcones) were designed, synthesized, and evaluated as α-glucosidase inhibitors (AGIs) with 1-deoxynojirimycin as positive control in vitro. Most of the compounds with two or four hydroxyl groups showed better inhibitory activities than 1-deoxynojirimycin towards α-glucosidase with noncompetitive mechanism. Moreover, most of the hydroxy bis-chalcones exhibit good α-glucosidase inhibitory activities in enzyme test. Inspiringly, bis-chalcones 2g (at 1 μM concentration) has stronger effect than 1-deoxynojirimycin on reducing the glucose level in HepG-2 cells (human liver cancer cell line).

Hydroxylated chalcones with dual properties: Xanthine oxidase inhibitors and radical scavengers

In this study, we evaluated the abilities of a series of chalcones to inhibit the activity of the enzyme xanthine oxidase (XO) and to scavenge radicals. 20 mono- and polyhydroxylated chalcone derivatives were synthesized by Claisen-Schmidt condensation reactions and then tested for inhibitory potency against XO, a known generator of reactive oxygen species (ROS). In parallel, the ability of the synthesized chalcones to scavenge a stable radical was determined. Structure-activity relationship analysis in conjunction with molecular docking indicated that the most active XO inhibitors carried a minimum of three hydroxyl groups. Moreover, the most effective radical scavengers had two neighboring hydroxyl groups on at least one of the two phenyl rings. Since it has been proposed previously that XO inhibition and radical scavenging could be useful properties for reduction of ROS-levels in tissue, we determined the chalcones' effects to rescue neurons subjected to ROS-induced stress created by the addition of β-amyloid peptide. Best protection was provided by chalcones that combined good inhibitory potency with high radical scavenging ability in a single molecule, an observation that points to a potential therapeutic value of this compound class.

COMPOUNDS FOR THE TREATMENT OF NEURODEGENERATIVE DISEASES

Compounds and their pharmaceutically acceptable salts for treatment of synucleinopathies, such as Parkinson's disease and tauopathies.

Synthesis and evaluation of 2′,4′,6′-trihydroxychalcones as a new class of tyrosinase inhibitors

In this study, we synthesized a series of hydroxychalcones and examined their tyrosinase inhibitory activity. The results showed that 2′,4′,6′-trihydroxychalcone (1), 2,2′,3,4′,6′-pentahydroxychalcone (4), 2′,3,4,4′,5,6′-hexahydroxychalcone (5), 2′,4′,6′-trihydroxy- 3,4-dimethoxychalcone (9) and 2,2′,4,4′,6′-pentahydroxychalcone (15) exhibited high inhibitory effects on tyrosinase with respect to l-tyrosine as a substrate. By the structure-activity relationship study, it was suggested that the 2′,4′,6′-trihydroxyl substructure in the chalcone skeleton were efficacious for the inhibition of tyrosinase activity. And also, the catechol structure on B-ring of chalcones was not advantageous for the inhibitory potency. Furthermore, 15 (IC50 = 1 μM) was found to show the highest activity out of a set of 15 hydroxychalcones, even better than both 2,2′,4,4′-tetrahydroxychalcone (13, IC50 = 5 μM) and kojic acid (16, IC50 = 12 μM), which were known as potent tyrosinase inhibitors. Kinetic study revealed that 15 acts as a competitive inhibitor of tyrosinase with Ki value of 3.1 μM.