190323-49-0

Upstream product

• 17912-87-7 myricetin 3-O-α-rhamnopyranoside 
• 74-88-4 methyl iodide 
• 529-44-2 myricetin 
• 17912-87-7 myricitrin 
• 77-78-1 dimethyl sulfate 
• 86-81-7 3,4,5-trimethoxy-benzaldehyde 
• 53350-26-8 5,7-Dimethoxy-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one 
• 53350-27-9 (E)-1-(2′-hydroxy-4′,6′-dimethoxyphenyl)-3-(3,4,5-trimethoxyphenyl)prop-2-en-1-one 
• 71660-27-0 3-hydroxy-5,7-dimethoxy-2-(3,4,5-trimethoxy-phenyl)-chroman-4-one 
• 186581-53-3 diazomethane 
• 110-46-3 isopentyl nitrite 

Downstream Products

• 14813-27-5 myricetin hexamethyl ether 

Relevant academic research and scientific papers

Synthesis and antibacterial activity of novel myricetin derivatives containing sulfonylpiperazine

Myricetin derivatives containing sulfonylpiperazine were synthesized and their structures were confirmed by NMR and HRMS. The antibacterial activity results indicated that some compounds showed good antibacterial activity against Xanthomonas oryzaepv. ory

Design, synthesis, and antibacterial activity of novel myricetin derivatives containing sulfonate

A series of myricetin derivatives containing sulfonate groups were designed and synthesized. Preliminary antibacterial activity showed that most of the target compounds exhibited significant biological activities against Xanthomonas axonopodis pv. Citri (Xac), Ralstonia solanacearum (Rs), and Xanthomonas oryzae pv. Oryzae (Xoo). In particular, the EC50 value of compound 3e was 13.76?μg/cm3 against Xac, which was better than commercial reagents bismerthiazol (50.32?μg/cm3) and thiodiazole copper. (83.27?μg/cm3), and the EC50 value of compound 3j was 11.92?μg/cm3 against Xoo in vitro, The result was better than that of bismerthiazol (72.08?μg/cm3) and thiodiazole copper (99.26?μg/cm3). Compound 3j displayed the better in vivo activity against rice bacterial leaf blight than bismerthiazol and thiodiazole copper. Meanwhile, the antibacterial mechanism of compounds 3e and 3j was studied by scanning electron microscope (SEM). These results suggested that myricetin derivatives containing sulfonate can be considered as a new antibacterial reagents. Graphic abstract: [Figure not available: see fulltext.]

Novel myricetin derivatives: Design, synthesis and anticancer activity

Telomere and telomerase were closely related to occurrence and development of some cancers. To enhance ability of myricetin moiety for inhibiting telomerase, we designed a series of novel myricetin derivatives based on reasonable analysis. The telomerase inhibition assay showed that compound 6d displayed the most potent inhibitory activity with IC50 value of 0.91 μM. The anticancer activity assay showed that 6d exhibited high activity against human breast cells MDA-MB-231. The docking simulation of compound 6d was performed to get the probable binding model, the results demonstrated that the furan ring inserted into the active site deeply and had hydrophobic interactions with residues of Phe 568, Pro 627, four methoxy groups had hydrophobic interactions with residues of Phe 568, Pro 627, Lys 902, Val 904 and Pro 929. Western blot results showed that expression of p65 and TERT protein was clearly down-regulated by compound 6d. These data support further studies for the rational design of more efficient p65 and TERT modulators.

Design and synthesis of the 4H-chromenone derivatives against psoriasis

On basis of Quercetin moiety, two series of 20 new compounds were designed and synthesized accordingly in this study, and their anti-inflammatory activities in vitro and in vivo were evaluated. At last, compound 8A2: 3- (1- (2- (4- (5-bromo-2-chlorobenzoyl) piperazin-1-yl) ethyl)-1H-1,2,3-triazol-4-yl) methoxy)-5,7-dimethoxy-2-(3,4,5-trimethoxyphenyl)-4H-chromen-4-one with low toxicity was found the best one for inhibiting of NO. Meanwhile, this compound could significantly inhibit the expression of IL-6 (Interleukin-6), TNF-α (Tumor necrosis factor-α) and IL-17 (Interleukin-17), and also significantly down-regulate IL-17 mRNA psoriasis model in vitro. Further studies were performed to establish mouse psoriasis model induced by Imiquimod (IMQ), and the preliminary mechanism indicated that compound 8A2 may alleviate mouse psoriasis through obstructed the JAK1/2-STAT1/3 pathway. This study should be provide a basis for further study of effective treatment of psoriasis.

Design, Synthesis and Antibacterial Activity of Novel Pyrimidine-Containing 4H-Chromen-4-One Derivatives**

A series of pyrimidine-containing 4H-chromen-4-one derivatives were designed and synthesized by combining bioactive substructures. Preliminary biological activity results showed that most of the compounds displayed significant inhibitory activities in vit

Pharmacokinetics and Metabolites of 12 Bioactive Polymethoxyflavones in Rat Plasma

Polymethoxyflavones (PMFs) are a subgroup of flavonoids possessing various health benefits. 3,5,7,4′-Tetramethoxyflavone (1), 5,6,7,4′-tetramethylflavone (2), 3,7,3′,4′-tetramethoxyflavone (3), 5,7,3′,4′-tetramethoxyflavone (4), 5-hydroxy-3,7,2′,4′-tetramethoxyflavone (5), 3,5,7,2′,4′-pentamethoxyflavone (6), 5-hydroxy-3,7,3′,4′-tetramethoxyflavone (7), 3-hydroxy-5,7,3′,4′-tetramethylflavone (8), 3,5,7,3′,4′-pentamethoxyflavone (9), 5-hydroxy-3,7,3′,4′,5′-pentamethoxyflavone (10), 3-hydroxy-5,7,3′,4′,5′-pentamethoxyflavone (11), and 3,5,7,3′,4′,5′-hexamethoxylflavone (12) were 12 bioactive and available PMFs. The aim of this study was to investigate the pharmacokinetic, metabolite, and antitumor activities as well as the structure-pharmacokinetic-antitumor activity relationships of these 12 PMFs to facilitate further studies of their medicinal potentials. The cytotoxicity of PMFs with a hydroxy group toward HeLa, A549, HepG2, and HCT116 cancer cell lines was generally significantly more potent than that of PMFs without a hydroxy group. Compounds 5, 7, 8, 10, and 11 were all undetectable in rat plasma, while compounds 1-4, 6, 9, and 12 were detectable. Both the number and position of hydroxy and methoxy groups played an important role in modulating PMF pharmacokinetics and metabolites.

Synthesis, telomerase inhibitory and anticancer activity of new 2-phenyl-4H-chromone derivatives containing 1,3,4-oxadiazole moiety

Based on previous studies, 66 2-phenyl-4H-chromone derivatives containing amide and 1,3,4-oxadiazole moieties were prepared as potential telomerase inhibitors. The results showed most of the title compounds exhibited significantly inhibitory activity on telomerase. Among them, some compounds demonstrated the most potent telomerase inhibitory activity (IC50 50 = 6.41 μM). In addition, clear structure–activity relationships were summarised, indicating that the substitution of the methoxy group and the position, type and number of the substituents on the phenyl ring had significant effects on telomerase activity. Among them, compound A33 showed considerable inhibition against telomerase. Flow cytometric analysis showed that compound A33 could arrest MGC-803 cell cycle at G2/M phase and induce apoptosis in a concentration-dependent way. Meanwhile, Western blotting revealed that this compound could reduce the expression of dyskerin, which is a fragment of telomerase.

Sulfonic ester-containing myricetin derivative, preparation method and application thereof

The invention discloses a sulfonic ester-containing myricetin derivative, a preparation method and application thereof, wherein the structural general formula is as shown in the specification. R is independently selected from one or more of C1-C6 alkyl radical, C1-C6 alkenyl radical, C1-C6 alkynyl group, halogen atom, C3-C6 cycloalkyl, optionally substituted or unsubstituted phenyl, and optionally substituted or unsubstituted aromatic heterocyclic group; substituted phenyl and substituted aromatic heterocyclic radical. The substituted phenyl is a benzene ringwith alkyl containing C1-6, alkoxy containing C1-6, nitro, halogen atom and hydrogen atom at ortho, meta and para positions; the aromatic heterocyclic group is thienyl, furyl, pyrrolyl and pyridyl; and the substituent on the substituted aromatic heterocycle is alkyl containing C1-6, alkoxy containing C1-6, nitro, halogen atom and hydrogen atom at ortho, meta and para positions; The sulfonic ester-containing myricetin derivative has good inhibitory activity on cancer cells.

Antimicrobial evaluation of myricetin derivatives containing benzimidazole skeleton against plant pathogens

A series of novel myricetin derivatives containing benzimidazole skeleton were constructed. The structure of compound 4g was further corroborated via X-ray single crystal diffractometer. The antimicrobial bioassays showed that all compounds exhibited potent inhibitory activities against Xanthomonas axonopodis pv. Citri (Xac), Ralstonia solanacearum (Rs) and Xanthomonas oryzae pv. Oryzae (Xoo) in vitro. Significantly, compound 4q showed the best inhibitory activities against Xoo, with the EC50 value of 8.2 μg/mL, which was better than thiodiazole copper (83.1 μg/mL) and bismerthiazol (60.1 μg/mL). In vivo experimental studies showed that compound 4q can treat rice bacterial leaf blight at 200 μg/mL, and the corresponding curative and protection efficiencies were 45.2 and 48.6%, respectively. Meanwhile, the antimicrobial mechanism of the compounds 4l and 4q were investigated through scanning electron microscopy (SEM). Studies showed that compounds 4l or 4q can cause deformation or rupture of Rs or Xoo cell membrane. These results indicated that novel benzimidazole-containing myricetin derivatives can be used as a potential antibacterial reagent.

Myricetin derivative containing benzimidazole sulfonamide as well as preparation method and application of myricetin derivative

The invention discloses a myricetin derivative containing benzimidazole sulfonamide as well as a preparation method and an application of the myricetin derivative, the structural general formula of the myricetin derivative is shown in the specification, i