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129results about How to "Strong in vitro antitumor activity" patented technology
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Synthesis of 9-chloro-1,2,3,4-tetrahydroacridine-platinum (II) complex targeted to liver cancer and application of the complex
ActiveCN107746418AGrowth inhibitionHas medicinal valuePlatinum organic compoundsAntineoplastic agentsChemical structurePlatinum
The invention discloses synthesis of a 9-chloro-1,2,3,4-tetrahydroacridine-platinum (II) complex targeted to liver cancer and an application of the complex and belongs to the technical field of medicines. The invention aims to provide a dichloro-dimethyl-sulfoxide-9-chloro-1,2,3,4-tetrahydroacridine-platinum (II) complex having a novel structure, and a synthesis method and an application thereof.The chemical structure formula of the dichloro-dimethyl-sulfoxide-9-chloro-1,2,3,4-tetrahydroacridine-platinum (II) complex is represented as follow. The complex can be used for producing antitumor medicines.
Owner:YULIN NORMAL UNIVERSITY
Gem-difluoro ethyl substitutional diphenylethene and diphenylethane derivative as well as preparation method and application thereof
ActiveCN107311846AStrong in vitro antitumor activityEnhanced antitumor activity in vitroOrganic compound preparationEther/acetal active ingredientsChemical structureInhibitory effect
The invention discloses gem-difluoro ethyl substitutional diphenylethene and diphenylethene diphenylethane derivatives as well as a preparation method and application thereof. A 4' bit of a B aromatic ring of diphenylethane / diphenylethene is subjected to chemical structure modification through gem-difluoro ethyl, and meanwhile, a 2' bit is modified into nitro or an amino group and other substituent groups; the gem-difluoro ethyl substitutional diphenylethene and diphenylethane derivative has relatively high antitumor activity in vitro, and the antitumor activity of a trans-form is better than the antitumor activity of a cis-form; with the introduction of fluorine atoms, not only is the physical property of the compound changed, but also the antitumor activity in vitro is improved at the same time, and the derivative has a relatively good inhibiting effect on multiple tumor cells.
Owner:SHANGHAI ECUST BIOMEDICINE CO LTD
7-substituted-4-aryl coumarins compound, and preparation method and application thereof
ActiveCN106674176AStrong inhibitory activityStrong in vitro antitumor activityOrganic chemistryAntineoplastic agentsArylSynthesis methods
The invention discloses a 7-substituted-4-aryl coumarins compound, and a preparation method and an application thereof and belongs to the technical field of antitumor drugs. The 7-substituted-4-aryl coumarins compound is acquired in the manner of modifying and remolding 4 and 7 loci of the coumarins. The structural formula is shown in the specification. A pharmacological experiment proves that such a compound has an excellent antitumor activity, can be used for preparing the antitumor drugs, is capable of supplying a new selection for the development and application of the antitumor drugs and further can be applied to the design and optimization of the antitumor drugs. The preparation method of the compound has the advantages of easily acquired raw materials, mild reaction condition, easily realized synthesis method, simple reaction process and operation, low-cost reagents and higher yield.
Owner:XI AN JIAOTONG UNIV
Preparing method of sea anemone crude extract and anti-tumor application of sea anemone crude extract
InactiveCN105030838ARetain biological activityStrong in vitro antitumor activityAntineoplastic agentsCnidaria material medical ingredientsFreeze-dryingMicrobiology
The invention relates to a preparing method of sea anemone crude extract. The preparing method includes the steps of 1, washing bred live sea anemones in pure water, placing the washed sea anemones in a beaker, adding pure water into the beaker according to a sea anemone to pure water ratio being 1:1.5 to 1:2, and performing freeze thawing twice to three times at -60 DEG C; 2, moderately unfreezing the sea anemones obtained in the step 1, and performing coarse filtration; 3, centrifuging filtrate obtained in the step 2 at 4 DEG C to 6 DEG C at the speed of 12000-14000 r / min for 10 to 15 min, and collecting supernate to obtain sea anemone crude venom; 4, subjecting the sea anemone crude venom obtained in the step 3 to fractional precipitation with acetone, centrifuging precipitate obtained in each step for 15min, collecting final precipitate, and freeze-drying the final precipitate to obtain sea anemone crude toxin. The invention further provides application of the sea anemone crude toxin in the preparation of anti-lung cancer medicaments.
Owner:ZHEJIANG OCEAN UNIV
Trans-diaryl ethylene LSD1 (lysine specific histone demethylase 1) inhibitor, as well as preparation method and application thereof
ActiveCN107501169AStrong LSD1 inhibitory activityStrong in vitro antitumor activityOrganic chemistryAntineoplastic agentsLead compoundDrug
The invention discloses an LSD1 (lysine specific histone demethylase 1) inhibitor with a trans-diaryl ethylene structure, as well as a preparation method and application thereof in preparation of an anti-tumour medicament, and belongs to the technical field of medicinal chemistry. The compound disclosed by the invention has a general formula which is as shown in the description; in-vitro LSD1 enzyme inhibiting activity and anti-tumour activity experiments prove that the compound has an obvious inhibiting effect on tumour cells by inhibiting the activity of LSD1, can serve as a lead compound for further development, and is applied to preparation of anti-tumour medicaments.
Owner:XINXIANG MEDICAL UNIV
Arginine-substituted phthalocyanine derivatives, and synthesis method and application thereof
ActiveCN106083866AGood photosensitive anti-tumor activityStrong ability to generate active oxygenOrganic chemistryEnergy modified materialsPhotodynamic therapyArginine
The invention discloses arginine-substituted phthalocyanine derivatives and a synthesis method thereof, and application of the arginine-substituted phthalocyanine derivatives in photodynamic therapeutics. The structure of the arginine-substituted phthalocyanine derivatives is disclosed as the following formula in the specification. The synthesis method of the arginine-substituted phthalocyanine derivatives is simple, and does not need any toxic methylation reagent; and the arginine-substituted phthalocyanine derivatives are positively charged under physiological conditions, have the advantages of high active oxygen generation capacity, favorable photosensitive antineoplastic activity and low dark toxicity, and thus, have favorable application prospects in photodynamic therapeutics.
Owner:NANJING NORMAL UNIVERSITY
Water-soluble o-nitrophenol-containing copper porphyrin and Schiff base copper porphyrin complex thereof, and synthesis method and application thereof
ActiveCN106854210AImprove hydrophilicityAvoid defectsOrganic active ingredientsGroup 1/11 organic compounds without C-metal linkagesSolubilitySynthesis methods
The invention discloses water-soluble o-nitrophenol-containing copper porphyrin and a Schiff base copper porphyrin complex thereof, and a synthesis method and an application thereof, and belongs to the field of chemical application. The synthesis method of THE o-nitrophenol-containing copper porphyrin and the Schiff base complex thereof is disclosed by using functional group modification as a main means. The application of the water-soluble o-nitrophenol-containing copper porphyrin and the Schiff base copper porphyrin complex thereof in biological activity, including the interaction of calf thymus DNA (ct-DNA) and in-vitro antitumor researches, is introduced. A pyridyl cation is introduced to a porphyrin ring through modification, so the hydrophilicity of lipophilic porphyrin compounds is greatly increased; and the increase of the solubility overcomes a severe defect of the porphyrin derivatives, so the anticancer performance is significantly increased. A result of the study of the application shows that the water-soluble o-nitrophenol-containing copper porphyrin and the Schiff base complex thereof have good in-vitro antitumor activity.
Owner:NORTHWEST UNIVERSITY FOR NATIONALITIES
Synthetic method of oxidized nantenine and application of oxidized nantenine
InactiveCN104387399AProliferation inhibitory activityStrong in vitro antitumor activityOrganic active ingredientsOrganic chemistryAcetic acid3,4-Dimethoxyphenethylamine
The invention discloses a synthetic method of oxidized nantenine and application of the oxidized nantenine. The synthetic method of the oxidized nantenine comprises the following steps: taking 2-(benzo[d][1,3]dioxol-5-yl)acetic acid and 3,4-dimethoxy phenethylamine as starting materials, and conducting seven-step reaction to synthesize the oxidized nantenine. Compared with the prior art, the organic complete synthetic method of the oxidized nantenine is provided by the invention; experiments indicate that the oxidized nantenine has a proliferation inhibitory activity against a plurality of human tumor cell strains, shows up a good antitumor activity in vitro, is excellent in potential medicinal value, and can be applied to preparation of various anti-tumor drugs.
Owner:GUANGXI NORMAL UNIV
Camptothecin type medicine loaded on high molecular nano-microsphere, and its prepn. method
InactiveCN1861192AObvious sustained release characteristicsStrong in vitro antitumor activitySolution deliveryPharmaceutical non-active ingredientsPolyesterMedicine
A camptothecine kind of medicines carried by high-molecular nanospheres for intravenous injection is composed of the biodegradable high-molecular nanospheres prepared from polyester or polyester-polyethanediol block copolymer and at least one camptothecine medicine (30 mass%). Its preparing process is also disclosed.
Owner:NANJING UNIV
Multi-targeted anti-tumor activity evodiamine derivative and preparation method and application thereof
PendingCN110066281AStrong in vitro antitumor activityExcellent in vivo tumor growth inhibitory activityNervous disorderOrganic chemistryEvodiamineDNA underwinding
The invention belongs to the technical field of medicine, and provides a multi-targeted micromolecular anti-cancer drug based on topoisomerase 1 (Top1), topoisomerase 2 (Top2) and histone deacetylase(HDAC) and a preparation method of the multi-targeted micromolecular anti-cancer drug. The general molecular formulas of the compound are shown in the formulas I and II. Through pharmacological experiments, it is shown that the compound has high inhibitory activity to the topoisomerase 1, the topoisomerase 2 and the histone deacetylase, and has high in-vitro anti-tumor activity and excellent in-vivo anti-tumor effects. The invention further provides a preparation method of the derivative and application of the derivative in preparing a topoisomerase inhibitor, a histone deacetylase inhibitor and the anti-tumor drug.
Owner:SECOND MILITARY MEDICAL UNIV OF THE PEOPLES LIBERATION ARMY
Zinc phthalocyanine hydriodate photosensitizer, as well as preparation method and application thereof
InactiveCN105315289AProcess stabilityStrong absorption capacityOrganic chemistryEnergy modified materialsSolubilityProtonation
The invention discloses a 2,9,16,23-tetra-((4-aminomethyl) phenoxy) zinc phthalocyanine hydroiodide, as well as a preparation method and application thereof to a photodynamic therapy method, and relates to a 2,9,16,23-tetra-((4-aminomethyl) phenoxy) zinc phthalocyanine hydroiodide photosensitizer. The 2,9,16,23-tetra-((4-aminomethyl) phenoxy) zinc phthalocyanine hydroiodide photosensitizer not only is simple in synthetic method, excellent in solubility (based on the protonation principle) in water, high in anti-tumor activity (based on the heavy atom effect) and low in dark toxicity, but also has a good application prospect in the field of photodynamic therapy methods.
Owner:NANJING NORMAL UNIVERSITY
Copper chloride complex using 1-(2-pyridine)-9-hexyl-beta-carboline as ligand and synthesis method and application thereof
ActiveCN106632424AStrong in vitro antitumor activityGood potential medicinal valueOrganic active ingredientsGroup 1/11 organic compounds without C-metal linkagesN dimethylformamideSynthesis methods
The invention discloses a copper chloride complex using 1-(2-pyridine)-9-hexyl-beta-carboline as a ligand and a synthesis method and application thereof. A structural formula of the complex is shown as the following formula (I). The synthesis method comprises the steps that the compound shown as a following formula (II) and copper chloride are taken and dissolved in a polar solvent to perform complexing reaction, wherein the polar solvent is selected from one or more of methyl alcohol and ethyl alcohol and one or more of water, acetone, chloroform, dichloromethane and N,N-dimethylformamide. The complex shows the stronger antitumor activity than the ligand and cis-platinum, has a good potential medicinal value and is hopeful for preparation of various antitumor drugs. The structures shown by the formulas (I) and (II) are shown in the description.
Owner:GUANGXI NORMAL UNIV
Drug for preventing and treating bronchogenic carcinoma and preparation method thereof
InactiveCN108586443AStrong in vitro antitumor activityEnhanced inhibitory effectOrganic active ingredientsOrganic chemistryInhibitory effectAntitumor activity
The invention relates to a drug for preventing and treating bronchogenic carcinoma and a preparation method of the drug. The compound has good in-vitro antitumor activity, and has obvious inhibition effect for human lung cancer cell A-549 and non-small cell lung cancer NSCLC, compared with known anticancer drugs, the inhibition effect is equivalent or more prominent, and the drug is suitable for being used for preventing or treating bronchogenic carcinoma, especially for primary bronchogenic carcinoma.
Owner:佳木斯大学附属第一医院
PARP (poly-ADP-ribose polymerase)-1 and PI3K (phosphatidylinositol-3-kinase) dual target inhibitors containing phthalazine-1(2H)-ketone structure
ActiveCN109810098AStrong in vitro antitumor activityPrevent proliferationOrganic active ingredientsOrganic chemistryTriazinePhosphatidylinositol 3-Kinases
The invention relates to the field of medicinal chemistry, and specifically relates to a kind of PARP (poly-ADP-ribose polymerase)-1 and PI3K (phosphatidylinositol-3-kinase) dual target inhibitors (I)containing phthalazine-1(2H)-ketone and triazine or pyrimidine structures, preparation methods of the inhibitors, as well as pharmaceutical compositions containing compounds. It is proved, by pharmacodynamic tests, that the compounds involved in the invention have anti-tumor effects. The dual target inhibitors (I) are shown in the description.
Owner:CHINA PHARM UNIV
Water-soluble nitryl-containing copper porphyrin and water-soluble Schiff base copper porphyrin complex thereof, as well as synthesis methods and application of water-soluble nitryl-containing copper porphyrin and water-soluble Schiff base copper porphyrin complex thereof
InactiveCN107987085AStrong in vitro antitumor activityImprove hydrophilicityOrganic active ingredientsGroup 1/11 organic compounds without C-metal linkagesSolubilitySynthesis methods
The invention dislcoses synthesis methods and bioactive application of nitryl-containing copper porphyrin and a Schiff base copper complex thereof, and belongs to the field of chemical application. Firstly the synthesis methods of the nitryl-containing copper porphyrin and the Schiff base copper complex thereof are introduced by taking functional group modification as a main means; secondly the bioactive application is introduced, including research on mutual action of the nitryl-containing copper porphyrin and calf thymus DNA (CT-DNA) and in-vitro tumor resisting. Moreover, pyridyl cation isintroduced onto a porphyrin ring by means of modification, hydrophilicity of an oleophilic porphyrin compound is greatly increased, the increasement of solubility overcomes a great defect of a porphyrin derivative, so that the cancer resistance of the porphyrin derivative is remarkably improved. Through the research on mutual action of the nitryl-containing copper porphyrin and the calf thymus DNAand in-vitro tumor resisting, it is preliminarily considered that the synthesized novel water-soluble nitryl-containing copper porphyrin and the Schiff base copper complex thereof have better in-vitro anti-tumor activity.
Owner:NORTHWEST UNIVERSITY FOR NATIONALITIES
Anti-tumor bipyridine methyl substituted manganese amino acid complex, and preparation and application thereof
InactiveCN101412737AGood antitumor effectImprove anti-tumor effectOrganic active ingredientsAntineoplastic agentsModel compositionManganese
The invention relates to a novel targeted antitumor small molecular compound and the technical field of preparation thereof, in particular to a targeted antitumor bipyridine methyl substituted aminophenol manganese composition, a preparation method and application thereof. Two new chiral bipyridine methyl substituted aminophenol compounds (L-model) and four new bipyridine methyl substituted aminophenol ligand manganese compositions are synthesized through a chemical method; and a structure of the composition is determined by a physical means. An in-vitro antitumor activity test researches the influence of the composition on tumor cells and finds out that the manganese composition with small lipin distribution coefficient has strong inhibiting function on the growth of the tumor cells of A549, Hela, HepG-2 and Eca109; and the manganese composition synthesized by the L-model compositions has stronger capacity for identifying the tumor cells. Data of an animal test of the manganese composition show that the composition has good tumor inhibiting function. The manganese composition and mitochondria have direct action; and the new manganese composition can be used as a new antitumor activity medical composition with the mitochondria as a target spot.
Owner:JIANGSU UNIV
Copper nitrate complex taking 1-(2-pyridine)-9-benzyl-beta-carboline as ligand as well as synthesis method and application of copper nitrate complex
ActiveCN106478692AStrong in vitro antitumor activityGood potential medicinal valueOrganic active ingredientsGroup 1/11 organic compounds without C-metal linkagesN dimethylformamideSynthesis methods
The invention discloses a copper nitrate complex taking 1-(2-pyridine)-9-benzyl-beta-carboline as a ligand as well as a synthesis method and an application of the copper nitrate complex. The structural formula of the complex is shown in the following formula (I). The synthesis method of the complex comprises the steps as follows: the compound as shown in the following formula (II) and copper nitrate are taken and dissolved in a polar solvent for a coordination reaction, and the copper nitrate complex is obtained, wherein the polar solvent is a combination of one or two selected from methanol and ethanol with one or more than two selected from water, acetone, chloroform, dichloromethane and N, N-dimethylformamide. The complex exhibits higher antitumor activity than the ligand and cisplatin, has better potential medicinal value and is expected to be used for preparation of various antitumor drugs. The structures in the formula (I) and the formula (II) are shown in the specification.
Owner:GUANGXI NORMAL UNIV
Copper nitrate complex of 1-(2-pyridine)-9-(4-methylbenzyl)-beta-carboline and synthesizing method and application of copper nitrate complex
ActiveCN106632421AStrong in vitro antitumor activityGood potential medicinal valueOrganic active ingredientsCopper organic compoundsDimethyl formamideDichloromethane
The invention discloses a copper nitrate complex of 1-(2-pyridine)-9-(4-methylbenzyl)-beta-carboline and a synthesizing method and application of the copper nitrate complex. The structural formula of the complex is as shown in formula (I). The synthesizing method includes: dissolving a compound as shown in formula (II) and copper nitrate into a polar solvent to perform complexing reaction so as to obtain the copper nitrate complex, wherein the polar solvent is formed by combining one or two of methanol and ethanol with one or more than two of water, acetone, chloroform, dichloromethane and N,N-dimethyl formamide. The copper nitrate complex has higher antitumor activity as compared with those of ligands and cis-platinum, has a good potential medicinal value and can be hopefully used for preparing various antitumor drugs.
Owner:GUANGXI NORMAL UNIV
Copper chloride complex by taking 1-(2-pyridine)-9-butyl-beta-carboline as ligand as well as synthetic method and application of complex
ActiveCN106632420AStrong in vitro antitumor activityGood potential medicinal valueGroup 1/11 organic compounds without C-metal linkagesOrganic active ingredientsStructural formulaPharmaceutical Substances
The invention discloses a copper chloride complex by taking 1-(2-pyridine)-9-butyl-beta-carboline as a ligand as well as a synthetic method and application of the complex. The structural formula of the complex is shown as the following formula (I). The synthetic method comprises the following steps: taking a compound shown as a formula (II) and copper chloride, dissolving in a polar solvent, and carrying out a coordination reaction, thereby obtaining the product, wherein the polar solvent is selected from a combination of one or two of methanol and ethanol and one or more than two of water, acetone, chloroform, dichloromethane and N,N-dimethyl formamide. The complex disclosed by the invention has the antitumor activity higher than that of the ligand and cis-platinum, has excellent potential medicinal value and is expected to be used for preparing various antitumor medicines. The structures of the formulas (I) and (II) are shown in the specification.
Owner:GUANGXI NORMAL UNIV
Cereus sinensis verrill soluble cell peptide CCT-I and separating and purifying method and application thereof
ActiveCN103408650AStrong in vitro antitumor activityHigh purityPeptide/protein ingredientsPeptide preparation methodsFiltrationChromatography column
The invention discloses a cereus sinensis verrill soluble cell peptide CCT-I and a separating and purifying method and an application thereof. The separating and purifying method comprises the following steps: after cereus sinensis verrill tentacle crude toxin is salted out and fractionally precipitated with ammonium sulfate, active sites are separated and purified through Sephadex G-100 and superdex 75 gel filtration chromatography columns in sequence, and the soluble cell peptide is obtained through separation from a cereus sinensis verrill tentacle at the first time and is finally authenticated as the novel cereus sinensis verrill soluble cell peptide that has not been reported through SDS-PAGE and LC-MS, wherein two peptides (alpha and beta) in the novel cereus sinensis verrill soluble cell peptide are similar in molecular weight of about 80 kDa, and the HPLC test shows that the two peptides are high in purify and similar in polarity. The half soluble cell rate is tested to be 5.75 micrograms*mL<-1>, and the MTT process test displays that the CCT-I has strong antitumor activity in vitro, and can be used for preparing tumor-treating drug.
Owner:张朝晖
Fluorine-containing AZD9291 derivative as well as preparation method and application thereof
InactiveCN110684016AChange physical propertiesEnhanced inhibitory effectOrganic chemistryAntineoplastic agentsOncologyResistance mutation
The invention relates to a fluorine-containing AZD9291 derivative as well as a preparation method and application thereof. The derivative has a structure of a formula (I) shown in the description, inthe formula, R1 is -CF2H or -CH3; R2 is -CF2H or -CH3; and at least one of R1 and R2 is -CF2H. Compared with the prior art, the derivative is capable of improving the in-vitro anti-tumor activity, hasa good inhibition function on multiple tumor cells, is capable of inhibiting activation or resistance mutation of EGFRs (epidermal growth factor receptors), is applied to treatment on EGFR sensitivemutation cancer, and is an ideal treatment medicine for diseases caused by EGFR mutation.
Owner:SHANGHAI INST OF TECH
Sulphated compound microalgae polysaccharide and preparation method and application thereof
ActiveCN107573433AInhibition of proliferation in vitroGrowth inhibitionOrganic active ingredientsAntineoplastic agentsSolubilityIn vitro proliferation
The invention relates to sulphated compound microalgae polysaccharide. The sulphated compound microalgae polysaccharide is prepared by mixing sulphated chlorella polysaccharide and sulphated spirulinaon the base of the ratio of 1 to 16-16 to 1. The sulphated compound microalgae polysaccharide is capable of effectively inhibiting in-vitro proliferation of tumor cells, and is high in water solubility, so that the sulphated compound microalgae polysaccharide can play a role in vitro and is capable of inhibiting the growth of tumor.
Owner:TIANJIN UNIVERSITY OF SCIENCE AND TECHNOLOGY
A kind of 7-substituted-4-aryl coumarin compound and its preparation method and application
ActiveCN106674176BStrong inhibitory activityStrong in vitro antitumor activityOrganic chemistryAntineoplastic agentsArylSynthesis methods
The invention discloses a 7-substituted-4-aryl coumarins compound, and a preparation method and an application thereof and belongs to the technical field of antitumor drugs. The 7-substituted-4-aryl coumarins compound is acquired in the manner of modifying and remolding 4 and 7 loci of the coumarins. The structural formula is shown in the specification. A pharmacological experiment proves that such a compound has an excellent antitumor activity, can be used for preparing the antitumor drugs, is capable of supplying a new selection for the development and application of the antitumor drugs and further can be applied to the design and optimization of the antitumor drugs. The preparation method of the compound has the advantages of easily acquired raw materials, mild reaction condition, easily realized synthesis method, simple reaction process and operation, low-cost reagents and higher yield.
Owner:XI AN JIAOTONG UNIV
Copper chloride complex with 1-(2-pyridinyl)-9-ethyl-beta-carboline ligand and preparation method and application thereof
ActiveCN106478687AStrong in vitro antitumor activityGood potential medicinal valueOrganic active ingredientsGroup 1/11 organic compounds without C-metal linkagesCoordination complexMethanol
The invention discloses a copper chloride complex with 1-(2-pyridinyl)-9-ethyl-beta-carboline ligand and a preparation method and application thereof. The structure of the complex is represented as a formula (I), and the preparation method comprises the following steps: copper chloride and a compound of a formula (II) are dissolved in a polar solvent for a coordination reaction and then the product is obtained, wherein the polar solvent is a combination consisting of one or both selected from methanol and ethanol and one or more selected from water, acetone, chloroform, dichloromethane and N,N-dimethyformamide. The complex exhibits a higher antitumor activity than that of the ligand and cisplatin, has a better potential medicinal value and is hopeful to prepare a plurality of antitumor drugs. The structures of formulas (I) and (II) are shown in the description.
Owner:GUANGXI NORMAL UNIV
Tripterine derivate and use thereof
InactiveCN101805390BStrong in vitro antitumor activityImprove protectionOrganic active ingredientsNervous disorderTriptosineCentral nervous system
The invention discloses a tripterine derivate and use thereof. The tripterine derivate has a structure as shown by a formula I. When R2 is H, R1 is alkyl, amine radical, alcohol, aryl, mixed aryl or heterocyclic radical connected with tripterine through ester bonds or amido bonds, and R2 is acyl or organic acid radical when R1 is OH. The tripterine derivate can be used for preparing anticancer medicine, anti-inflammatory medicine or medicine for treating central nervous system diseases. The medicine can be made into tablets, capsules, granules, fine grains, powder, pills, plaser, oral liquid or injections.
Owner:JINAN UNIVERSITY
Ursdic acid isatin amide derivatives as well as preparation method and application thereof
ActiveCN110759961AStrong in vitro antitumor activityHas antitumor activitySteroidsAntineoplastic agentsPharmacometricsPharmaceutical drug
The invention discloses ursdic acid isatin amide derivatives as well as a preparation method and application thereof. The invention discloses ursdic acid isatin amide derivatives I-a to I-I with structures as shown in a general formula (I) and pharmaceutically acceptable salts thereof. The ursdic acid isatin amide derivatives and the pharmaceutically acceptable salts thereof disclosed by the invention have remarkable antitumor activity, and proven by pharmacological experiments, the ursdic acid isatin amide derivatives disclosed by the invention have an obvious effect on inhibiting human hepatoma cells HepG2 and SMMC-7721 and have the potential of developing antitumor drugs.
Owner:NANJING FORESTRY UNIV
Dihydro pyrrolidone derivative and application of same in preparing antitumor drugs
InactiveCN107652218AEasy to manufactureMild reaction conditionsOrganic active ingredientsOrganic chemistryDiseaseStructural formula
The invention provides a dihydro pyrrolidone derivation and an application of the same in preparing antitumor drugs. The structural formula of the dihydro pyrrolidone derivative is as indicated in theformula I, wherein R<1> refers to an aromatic base, alkyl or heterocyclic radical; R<2> refers to alkoxy, amino or secondary amino; R<3> refers to amino, secondary amino, alkoxy, aryloxy, alkyl sulphanyl, aromatic sulfur or nitrogenous heterocyclic radical. The provided compound has remarkable inhibitory effect on tumor cells especially growth of human breast cancel cells, human colon cancer cells, human cervical cancer cells and human lung cancer cells, high characteristics of antitumor activity in vitro and broad spectrum antitumor are represented, and the dihydro pyrrolidone derivation canbe applied to prevention and treatment of multiple tumor diseases of breast cancer, colon cancer, cervical cancer, lung cancer and the like in a manner of being individually or combined with other drugs. The preparation process of the compound is simple and easy to implement, reaction conditions are moderate, raw materials for reaction are easy to obtain, industrialization is easy to realize, andwide application value is achieved.
Owner:SOUTHERN MEDICAL UNIVERSITY
Fluorine-substituted diphenylethane compound and preparation method and application thereof
ActiveCN110240539AStrong in vitro antitumor activityEnhanced inhibitory effectAntibacterial agentsSenses disorderHydrogenBiological property
The invention relates to a fluorine substituted diphenylethane compound, which is characterized in that the structure is shown as a general formula (I): wherein R1 is methyl or ethyl; R2 is hydrogen or fluorine; and R is hydrogen, hydroxyl, benzyloxy, phosphate and phosphate salt. Compared with the prior art, fluorine substitution modification is performed on the bridge bond of diphenylethane, and the obtained fluorine substituted diphenylethane compound has stronger in vitro anti-tumor activity, the introduction of fluorine atoms changes the physical, chemical and biological properties of the compound, and the fluorine substituted diphenylethane compound has obvious inhibition effect on tumor cells. The preparation conditions are simple and easy to operate, and by-products are less.
Owner:SHANGHAI INST OF TECH +1
A class of diarylethene lsd1/hdacs dual-target inhibitors containing hydroxamic acid group, preparation method and application thereof
ActiveCN111592487BStrong dual inhibitory activityHigh activityOrganic compound preparationCarboxylic acid esters preparationHydroxamic acidHuman gastric carcinoma
Owner:XINXIANG MEDICAL UNIV
Oxonantenine rare-earth complex as well as synthesis method and application thereof
InactiveCN104447821AGood antitumor activityStrong in vitro antitumor activityOrganic active ingredientsGroup 3/13 organic compounds without C-metal linkagesSynthesis methodsRare earth
The invention discloses an oxonantenine rare-earth complex as well as a synthesis method and an application thereof. The rare-earth complex is obtained from a coordination reaction between oxonantenine which serves as a ligand and rare-earth metal salt in a polar solvent, and specifically, the rare-earth complex can be synthesized by virtue of a solution method or a solvothermal method. By investigating the inhibitory effect of the complex on the growth of multiple tumor cell strains, the applicant discovers that the rare-earth complex shows better antitumor activity in vitro than that of cis-platinum as a classical metal-based anti-cancer drug; meanwhile, some rare-earth complex also shows better antitumor activity in vitro than that of an oxonantenine ligand; and therefore, the rare-earth complex has a potential medicinal value, and is expected to be used for preparing various anti-cancer drugs. The structure of the rare-earth complex is as shown in formula I (as shown in Specification).
Owner:GUANGXI NORMAL UNIV
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