1355483-79-2

Upstream product

• 642-71-7 3,4,5-trimethoxyphenol 
• 22248-14-2 6-hydroxy-2,3,4-trimethoxyacetophenone 
• 1200-07-3 3-(4-bromophenyl)acrylic acid 
• 13565-09-8 4-bromocinnamoyl chloride 
• 1355483-74-7 2-(4-bromophenyl)-5,6,7-trimethoxy-4H-chromen-4-one 
• 1355483-83-8 C₁₈H₁₇BrO₅ 

Relevant academic research and scientific papers

4′-Bromo-5,6,7-trimethoxyflavone represses lipopolysaccharide-induced iNOS and COX-2 expressions by suppressing the NF-κB signaling pathway in RAW 264.7 macrophages

The regulations of the NO and PGE2 productions are research topics of interest in the field of anti-inflammatory drug development. In the present study, 5,6,7-trimethoxy- and 5,6,7-trihydroxyflavones 3a-3g were synthesized from cinnamic acid derivatives. In particular, 4′-bromo-5,6,7- trimethoxyflavone (3b) most potently inhibited the productions of NO and PGE2 in LPS-treated RAW 264.7 cells (IC50 = 14.22 ± 1.25 and 10.98 ± 6.25 μM, respectively), and these inhibitory effects were more potent than those of oroxylin A or baicalein. Consistent with these findings, 3b concentration-dependently reduced the LPS-induced expressions of iNOS and COX-2 at the protein and mRNA levels. In addition, the release of TNF-α, IL-6, and IL-1β and the mRNA expressions of these cytokines were reduced by 3b in a concentration-dependent manner. Furthermore, 3b attenuated the LPS-induced transcriptional activities of NF-κB and this was accompanied by parallel reductions in the degradation and phosphorylation of IκB-α, and consequently by a decrease in the nuclear translocation of the p65 subunit of NF-κB. Taken together, these results suggest that suppressions of the expressions of iNOS, COX-2, TNF-α, IL-6, and IL-1β via NF-κB inactivation are responsible for the anti-inflammatory effects of 3b.

Baicalein or derivative thereof, preparation method and application of baicalein or derivative of baicalein

The invention discloses baicalein or a derivative thereof. The structure is shown in the specification, wherein R1 is hydrogen, alkyl, substituted or unsubstituted aryl; R2 is hydrogen, halogen, alkyl, alkoxy, substituted or unsubstituted amino, and subst

Baicalein derivative as well as preparation method and application thereof (by machine translation)

The invention discloses a baicalein derivative, structure as shown in the specification : In-flight, R1 A hydrogen, alkyl, is substituted or unsubstituted aryl ;R. 2 The hydrogen, halogen, alkyl, alkoxy, may be substituted or unsubst

Antibacterial Flavonoids from Medicinal Plants Covalently Inactivate Type III Protein Secretion Substrates

Traditional Chinese Medicines (TCMs) have been historically used to treat bacterial infections. However, the molecules responsible for these anti-infective properties and their potential mechanisms of action have remained elusive. Using a high-throughput

COMPOSITION AND METHOD FOR TREATING OR PREVENTING INFLUENZA VIRUS INFECTION

The present invention provides a pharmaceutical composition and method for treating or preventing influenza virus infection in a subject comprising administering the subject with a pharmaceutical composition comprising a pharmaceutically acceptable carrier and a therapeutically effective amount of compounds provided in this invention. In addition, the prevent invention provides new compounds for treating or preventing influenza virus infection.

Synthesis and anti-influenza activities of novel baicalein analogs

A series of novel flavones derivatives were synthesized based on modification of the active ingredients of a traditional Chinese medicine Scutellaria baicalensis GEORGI and screened for anti-influenza activity. The synthetic baicalein (flavone) analogs, especially with the B-rings substituted with bromine atoms, were much more potent than oseltamivir or ribavirin against H1N1 Tamiflu-resistant (H1N1 TR) virus and usually with more favorable selectivity. The most promising were 5b, 5c, 6b and 6c, all displaying an 50% effective concentration (EC50) at around 4.0-4.5 μM, and a selective index (SI=50% cytotoxic concentration (CC50)/EC 50)>70. For seasonal H3N2-infected influenza virus, both 5a and 5b with SI >17.3 indicated superior to ribavirin. The flavonoids having both not-naturally-occurring bromo-substituted B-rings and appropriate hydroxyls positioning on the A-rings might be critical in determining the activity and selectivity against H1N1-Tamiflu-resistant infected influenza viruses.