25 results about "Flavone derivatives" patented technology

The present invention discloses a dandelion flavonoid derivative, its preparation method, and application. The dandelion flavonoid derivative has the following molecular structure: The dandelion flavonoid derivative provided by the present invention has anti-inflammatory and lung nodule-removing effects, is simple to prepare, and has good biocompatibility, making it a promising new drug for eliminating lung nodules.

Disclosed is an anticancer composition using a flavone derivative. In the present invention, the flavone derivative exhibits cytotoxicity against: H827, H1299, H522, and A549, which are human non-small cell lung cancer cell lines; MCF-7, which is a human breast cancer cell line; and PANC-1, which is a human pancreatic cancer cell line, in a time-dependent manner and in a treatment concentration-dependent manner, and not only exhibits a synergistic effect when used in combination with other conventional anticancer agents, such as osimertinib, which is an anticancer agent targeting for lung cancer, tamoxifen, which is a hormone agent against breast cancer, and gemcitabine, which is a cytotoxic anticancer agent against pancreatic cancer, but also exhibits the effect of synergistically inhibiting the expression of HIF-1α when used alone or in combination with an existing anticancer agent.

The present invention provides a medicinal compound comprising a synthetic flavonoid derivative according to formula (I), which has a group at the C-3 position: wherein at least two of R2-R6 are H, and the rest are independently selected from: H, OH, R1, OR1, NO2, NH2, NHR1, F, Cl, Br, I; wherein R1 is a free radical. The present invention also provides dimerization, trimerization and tetramerization compounds, wherein two or more quercetin units are connected to a central linker (skeleton) via position 3 and a spacer. The medicinal compound can be used to treat malignant tumors, in particular malignant epithelial tumors, such as colon cancer, melanoma and / or squamous cell carcinoma of the skin, lung cancer, breast cancer, basal cell carcinoma (basal cell tumor). #imgabs0#

The invention discloses a flavone derivative as well as a microwave preparation method and application thereof, and belongs to the technical field of medicinal chemistry. Comprising the following steps: S1, carrying out diazotization transfer reaction on a 1-phenyl-2-acetone compound to prepare an alpha-diazocarbonyl compound; and S2, heating the alpha-diazocarbonyl compound and 3-hydroxyflavone in microwaves to react to prepare the flavone derivative. The scheme provided by the invention is suitable for realizing Wolff rearrangement reaction of alpha-diazo compounds and alcohol compounds in microwaves, does not need to use the traditional kettle reaction, catalyst and excessive substrate, and has the advantages of simple operation, rapid reaction, few byproducts, high yield, short time and wide substrate application range; and the prepared flavonoid ester compound has an excellent anti-cancer effect.

The invention discloses a flavone derivative delivery system of targeted EGFR (Epidermal Growth Factor Receptor) protein as well as a preparation method and application of the flavone derivative delivery system, and belongs to the technical field of medicinal chemistry. The flavonoid derivative HT11 with anti-A beta and antioxidant activity is synthesized firstly, the depolymerization effect of the flavonoid derivative HT11 on A beta 1-42 reaches up to 92.40%, and the flavonoid derivative HT11 has good blood-brain barrier permeability. Then, the HT11 is loaded by taking the graphene oxide quantum dot as a carrier to obtain the HT11 coated GOQDs, so that the defect of low solubility of the HT11 is effectively overcome, and the targeting property and the curative effect of the HT11 coated GOQDs can be enhanced. Experimental results show that the HT11-coated GOQDs effectively solve the problem of reduction of AD animal space learning and memory ability, and possibility is provided for application of the HT11-coated GOQDs in the field of biological medicine.

The application belongs to the field of pharmaceutical chemistry, and particularly relates to a solid dispersion of 3,5,7-trihydroxy flavone derivatives, a preparation method and application thereof. The 3,5,7-trihydroxy flavone derivatives and PEG are firstly ground to form a solid dispersion, and then hot melt extrusion is carried out, the hot melt temperature of the 3,5,7-trihydroxy flavone derivatives and PEG is reduced by controlling specific hot melt extrusion conditions, the stability of the drug is ensured, and the obtained solid dispersion can achieve a rapid dissolution effect in a dissolution medium, and the bioavailability is correspondingly improved.

The invention discloses a flavone derivative and a preparation method and application thereof, the structural formula of the flavone derivative is shown as a general formula I: # imgabs0, X is selected from CH and N, R1 is selected from H, # imgabs1, # imgabs2 and # imgabs3, and the compound can significantly inhibit activation of a cell signal transduction STAT3 signal under a low dosage. Experimental results show that the compound can significantly inhibit proliferation of cell strains of multiple tumors such as lymphoma, multiple myeloma, cervical cancer, breast cancer, gastric cancer, lung cancer and pancreatic cancer, and can specifically inhibit STAT3 signal activation and expression of a downstream target gene cyclinD1; therefore, the compound has a prospect of being developed into a targeted anti-tumor drug related to the STAT3 signal transduction pathway.

The invention relates to an application of a chloroflavone derivative as an anti-candida albicans drug. The invention provides an anti-Candida albicans infection agent, which is characterized in that the anti-Candida albicans infection agent takes a compound represented by a formula I and / or a pharmaceutically acceptable salt thereof as an active ingredient and is used for treating infectious diseases caused by Candida albicans.

The synthesis method comprises the following steps: adding a methylthio phenyl alkynone compound as shown in a formula (I), 2-bromo-2, 2-difluoro-N-aryl acetamide as shown in a formula (II) and DABSO as shown in a formula (III) into a reaction solvent, carrying out stirring reaction under the conditions of nitrogen protection and illumination, and carrying out filtering, washing and drying, thereby obtaining the methylsulfonyl thioflavone derivative as shown in the formula (I). The synthesis method comprises the following steps: adding a methylthio phenyl alkynone compound as shown in the formula (I), 2-bromo-2, 2-difluoro-N-aryl acetamide as shown in the formula (II) and DABSO as shown in the formula (III) into the reaction solvent; after the reaction is finished, the reaction liquid is subjected to post-treatment to obtain a target compound, namely the methylsulfonyl-containing thioflavone derivative with the anti-tumor activity, shown as a formula (IV), the reaction equation is # imgabs0, and DABSO is a bis (sulfur dioxide)-1, 4-diazabicyclo [2.2. 2] octane adduct; in the formula (I) and the formula (IV), R is selected from a bromine atom or a pyridine ring; r1 is selected from a cyano group, a halogen group or a thienyl group. The method has the advantages of simple operation process, cheap and easily available raw materials, mild reaction conditions, environmental protection, atom economy and high yield.

The invention relates to compound of formula (I): in particular flavonoid derivatives (quercetin and catechin derivatives), for use in the prevention and / or the treatment of a disease or disorder involving both carbonyl and oxidative stresses.

The present invention relates to the pyrrolidine substituted with flavone derivatives, represented by the compounds of Formula (I) or a pharmaceutically acceptable salt, a solvate, a stereoisomer or a diastereoisomer thereof for use in the treatment of cancers associated with human papillomavirus. The present invention also relates to the pharmaceutical compositions containing the compounds of Formula (I) for the treatment of cancers associated with human papillomavirus.

The utility model relates to essence sampling technical field discloses a kind of white orchid flavone derivative whitening essence sampling equipment, including sampling cylinder main part and protective shell, the output shaft of electric push rod is fixed with rubber plug block, the lower portion of hose is equipped with sleeve, the lower end outer wall of hose is sleeved with collar, the outer wall of sleeve is sleeved with locating ring, the inner wall of locating ring is embedded with magnetic sheet two, the outer wall of collar is embedded with magnetic sheet one, the utility model is provided with locating ring, convex strip, collar, guide strip, sleeve and push column, first push locating ring along the convex strip of sleeve outer wall inlaying sliding when operating, accurately remove it to target sampling scale position of scale table, collar is driven along sleeve inner wall stable sliding by push column, when collar slides to the corresponding position of locating ring, magnetic sheet two and magnetic sheet one produce adsorption force, simultaneously, dismounting link does not need to be assisted by tool, guarantee the accuracy of subsequent whitening active ingredient detection result.

The invention relates to a flavonoid derivative, a preparation method thereof and application of the flavonoid derivative as a staphylococcus aureus and methicillin staphylococcus aureus resistant agent. The invention provides an anti-staphylococcus aureus and methicillin-resistant staphylococcus aureus agent, which is characterized in that the anti-staphylococcus aureus and methicillin-resistant staphylococcus aureus agent is prepared from compounds 1-11 shown as a formula I and / or pharmaceutically acceptable salts of the compounds 1-11 and / or the pharmaceutically acceptable salts of the compounds 1-11 and the pharmaceutically acceptable salts of the compounds 1-11, and the anti-staphylococcus aureus and methicillin-resistant staphylococcus aureus agent is used for treating infectious diseases caused by staphylococcus aureus and methicillin-resistant staphylococcus aureus (MRSA).

The invention discloses a flavone derivative containing a sulfonamide structure and a preparation method and application of the flavone derivative, and the flavone derivative has the following general formula structure: # imgabs0. The flavone derivative containing the sulfonamide structure is based on a combination mode of the flavone derivative containing the sulfonamide structure and Keap1 protein, and is combined with computer-aided drug design to introduce a sulfonyl group on a flavone skeleton, so that the flavone derivative containing the sulfonamide structure is obtained. The hydrogen bond interaction between the compound and amino acid residues Arg415 and Ser508 in the binding pocket is enhanced; meanwhile, the aromatic structure can be deeply combined with a pocket to enhance the hydrophobic binding force with amino acid residues such as Tyr525 and Tyr334, the water solubility is improved, and the biological activity of the target compound for interfering the Keap1-Nrf2 protein interaction is further improved.

Use of a flavonoid derivative of formula I or a salt thereof in preparing a medicament for preventing and / or treating sarcopenia. The chemical structural formula of formula I is as follows, wherein R1 and R2 are monosaccharides or oligosaccharides composed of glucose (glc) and / or rhamnose (rha) combined in different amounts and manners.

The invention discloses a novel CYP1B1 enzyme degradation agent as well as a preparation method and application thereof, and particularly discloses a CYP1B1 enzyme targeted hydrophobic tag HyT degradation agent which comprises an affinity ligand, a hydrophobic tag and a connecting chain for connecting the affinity ligand and the hydrophobic tag, each of the affinity ligand and the hydrophobic tag comprises an alpha-naphthylflavone derivative; the connecting chain comprises a plurality of repetitive units, and the repetitive units are composed of ethylene glycol fragments or alkyl groups. The invention also discloses a preparation method of the hydrophobic tag HyT degradation agent and application of the hydrophobic tag HyT degradation agent or a pharmaceutical composition thereof. The novel CYP1B1 enzyme degradation agent provided by the invention has stronger CYP1B1 enzyme targeting capability, and can specifically target tumors, realize sensitization anti-PD-L1 monoclonal antibody immunotherapy and enhance the tumor immunotherapy effect.

The invention discloses a synthetic method of a natural product flavonoid compound, and belongs to the technical field of synthesis of flavone derivatives, the synthetic method comprises eight specific steps, the synthetic method adopts an artificial synthesis method to synthesize the flavonoid compound 6-methoxyl-4 ', 5, 6'-tetramethyl-4 ', 5'-tetramethyl-4 ', 5'-tetramethyl-4 ', 5'-tetramethyl-4 ', 5'-tetramethyl-4 '-tetramethyl-4', 5 '-tetramethyl-4' Compared with the prior art, the method provided by the invention has the advantages of high yield and low cost, and can replace the method for separating and preparing the compound from the plant, and the method provided by the invention can be used for preparing the compound from the plant in the presence of the 2, 3, 7-trihydroxy-8-(1 ''-(3'' '-methoxyl-4 '''-hydroxyphenyl) ethyl) isoflavone.

New genistein phosphate derivatives, pharmaceutical compositions containing them, and their medicinal uses.

This invention relates to the fields of chemistry and pharmaceutical compounds, specifically to a coumarin-flavonoid derivative, its preparation method, and its applications. The coumarin-flavonoid derivative is a compound with the structure shown in Formula I, or a pharmaceutically acceptable salt, solvent compound, enantiomer, diastereomer, tautomer, or mixture thereof in any proportion; wherein n is an integer from 5 to 11; and X is any one of Cl, Br, and I. This compound exhibits good antibacterial activity against Staphylococcus aureus and methicillin-resistant Staphylococcus aureus, with high yield and low cytotoxicity. Formula I

The invention relates to the technical field of medicine, in particular to a compound containing a nitric oxide (NO) donor or pharmaceutically acceptable salt, a preparation method of the compound or the pharmaceutically acceptable salt, a pharmaceutical composition of the compound or the pharmaceutically acceptable salt, and application of the compound or the pharmaceutically acceptable salt to treatment or prevention of ophthalmic intraocular hypertension related diseases and optic nerve injury related diseases.

The present application belongs to the technical field of pharmaceutical compound synthesis improvement, and particularly relates to a three-body co-drug compound with anti-aging function, a preparation method thereof and a pharmaceutical preparation composition. The three-body co-drug compound is connected by a dissociable flexible covalent bond and comprises an asymmetric skeleton molecule, an apparent reset and anti-inflammatory autophagy function molecule and a decharge tissue lock closed function molecule. The asymmetric skeleton molecule is 1-methylpyridinium-3,5-dicarboxylic acid chloride, the apparent reset and anti-inflammatory function molecule is a flavone derivative, and the decharge tissue lock closed function molecule is a tertiary amine alkaloid.

The invention discloses an iodinated flavone derivative electrochemical synthesis method, which comprises: adding a flavone derivative, potassium iodide and a solvent into an unseparated electrolytic bath, using a graphite rod as an anode and a platinum sheet as a cathode, stirring under the current condition of 10 milliamperes, and separating and purifying a reaction crude product to obtain the iodinated flavone derivative. The invention develops an electrochemical C-H iodination reaction of potassium iodide and flavone derivatives, a series of functionalized iodinated flavone derivatives can be constructed through simple operation, and compared with the traditional synthesis method, the method has the main advantages that: 1) the reaction condition is mild, and the reaction can be smoothly carried out at room temperature; the method has the advantages of simple operation, no need of nitrogen protection, no use of a chemical oxidant due to the fact that an electric oxidation method is used in the reaction, good tolerance of functional groups, high yield and short reaction time.

The application belongs to the technical field of natural medicine chemistry, and discloses flavone derivatives in Jinyunhuang, and a preparation method and application thereof.The flavone derivatives are separated from Jinyunhuang of the plant Dalbergia hupeana, and the heartwood of Jinyunhuang is extracted and concentrated to obtain extractum, the extractum is separated by silica gel column chromatography, gel column chromatography, and semi-preparative high performance liquid chromatography, and the flavone derivatives can be obtained.The application establishes an inflammation model by inducing RAW 264.7 cells with lipopolysaccharide (LPS), and confirms that the compound has good anti-inflammatory activity and can be used for preparing anti-inflammatory drugs.

New genistein phosphate derivatives, pharmaceutical compositions containing them, and their medicinal uses.

The invention discloses an application of poplatin in preparation of a medicine for preventing and / or treating pulmonary fibrosis, the poplatin is at least one of poplatin, a poplatin derivative or a plant extract containing the poplatin, and the poplatin derivative can be converted into the poplatin in vivo to play a role. The invention provides an application of poplatin as an active component in preparation of a medicine for preventing and / or treating pulmonary fibrosis. The poplatin is a medicine capable of intervening in a pulmonary fibrosis core pathway. According to the invention, the poplatin is used as an active component for preparing the medicine for preventing and / or treating pulmonary fibrosis for the first time.