188results about How to "Good potential medicinal value" patented technology

The invention discloses a new 1-azabenzanthrone-platinum (II) complex, i.e., monochloro.mono(dimethyl sulfoxide).mono(1-azabenzanthrone) platinum (II), as well as a synthesis method and an application thereof. The complex is prepared through the following steps: weighing equivalent amounts of 1-azabenzanthrone and dichloro-di(dimethyl sulfoxide) platinum (II); dissolving in a polar solvent; heating or performing reflux reaction to obtain a target product, wherein the synthesis can specifically be performed through a solution method or a solvothermal method. Investigation shows that the complex has anti-proliferative activity on human tumor cell strains such as HepG2, SK-OV-3, SK-OV-3 / DDP, BEL-7404, T-24 and HL-7702; the result shows that the complex has obvious in-vitro anti-tumor activity, has higher potential medicinal value and is expected to be used for preparing various anti-tumor medicaments. The chemical structural formula of the complex is shown in the specification.

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.

The invention discloses a new platinum (II) complex of 6-amino oxoisoaporphine, namely monochloro.dimethyl sulfoxide.6-amino oxoisoaporphine platinum (II), and a synthesis method and an application thereof. The complex is synthesized by the steps of dissolving 6-amino oxoisoaporphine and dichloro.di(dimethyl sulfoxide) platinum (II) in a polar solvent, and heating or carrying out a reflux reaction to obtain the target product; specifically the complex can be synthesized by a solution method, and can also be synthesized by a solvothermal method. Through investigation of proliferation inhibitory activity of the complex against HepG2, BEL-7404 and NCI-H460 and other human tumor cell strains, the complex is found to have significant in-vitro antitumor activity against the 3 kinds of tumor strains and have relatively good potential medicinal value, and is expected to be used in preparation of various antitumor medicines. The complex has the chemical structure represented by the following formula as described in the specification.

The invention discloses two halogenated 8-hydroxyquinoline platinum (II) complexes and a synthesis method and application thereof. The structures of the halogenated 8-hydroxyquinoline platinum (II) complexes are shown in the formula (I), and the synthesis method comprises the steps that an 8-hydroxyquinoline derivative and dichloro bis(dimethyl sulfoxide) platinum are taken and subjected to a coordination reaction in a polar solvent, and the halogenated 8-hydroxyquinoline platinum (II) complexes are obtained. It is shown through experiments carried out by an applicant that the halogenated 8-hydroxyquinoline platinum (II) complexes have good activity of inhibiting the proliferation of certain tumor cell strains and can selectively inhibit the growth of bladder cancer T-24 cells, and the apoptosis of the tumor cells is induced under the function of targetedly interfering with mitochondria; meanwhile, the toxicity of the complexes to human normal cells HL-7702 is low. The structures of the halogenated 8-hydroxyquinoline platinum (II) complexes and the structure of the 8-hydroxyquinoline derivative are shown in the following formulas (I) and (II) respectively, wherein the formulas (I)and (II) are shown in the description, and R1 represents Cl or Br.

The invention discloses a 2-aryl-1,3-dihydro-benzimidazol derivative as well as a synthesis method and application thereof. The synthesis method comprises the following steps: placing 4-nitro-o-phenylenediamine and 2,4-dichlorobenzaldehyde in an organic solvent for a reaction under the normal-temperature or heating condition; conducting suction filtration on the obtained reactant, so as to obtain a target crude product of the 2-aryl-1,3-dihydro-benzimidazol derivative. According to the research of the applicant in the anti-renal fibrosis and anti-chronic nephrosis activities of the 2-aryl-1,3-dihydro-benzimidazol derivative, namely a compound, the compound is remarkable in in-vitro anti-renal fibrosis activity, has a relatively high potential medicinal values, and is expected to be used for preparation of anti-renal fibrosis and anti-chronic nephrosis medicines. The compound has a chemical structure shown in the formula (I).

The invention discloses a novel platinum (II) coordination compound of an oxidation iso-aporphine alkaloid (namely mono-chloride-dimethylsulfoxide-6-hydroxide radical oxidation iso-aporphine platinum (II)) and a synthesizing method and application of the mono-chloride-dimethylsulfoxide-6-hydroxide radical oxidation iso-aporphine platinum (II). According to the coordination compound, 6-hydroxide radical oxidation iso-aporphine and dichloro-dimethylsulfoxide platinum (II) which are equal in amount of substance are weighed and dissolved in a polar solvent, and a target product is obtained after a heating reaction or a reflux reaction; in detail, a solution method can be used for synthesizing, and meanwhile a solvothermal method can be used for synthesizing. Proliferation inhibition, on HepG2, SK-OV-3, SK-OV-3 / DDP, BEL-7404, T-24 and other human tumor cell stains, of the coordination compound is investigated, the result shows that the novel platinum coordination compound has obvious anti-tumor activity in vitro and good potential medicinal value and is expected to be used for preparation of kinds of anti-tumor drugs. The chemical structural formula of the coordination compound is as follows (please find the formula in the specification).

The invention relates to a tryptanthrin copper complex with antitumor activity and a synthetic method thereof; the tryptanthrin copper complex with antitumor activity has a structure as shown below; the tryptanthrin copper complex has significant inhibitory effect on ovarian cancer cell line Skov3, has potential medicinal value, is expected to serve as a metal antitumor drug and belongs to the technical field of medicine.

The invention discloses high-activity tacrine-platinum (II) complexes and a synthesis method and application thereof, and relates to the technical field of medicine. The purpose of the invention is toprovide six high-activity tacrine-platinum (II) complexes having novel structures. The six high-activity tacrine-platinum (II) complexes have chemical structural formulas shown in the formulas 1 to 6. The high-activity tacrine-platinum (II) complexes can be used for preparation of antitumor drugs.

The invention discloses a platinum (II) complex, a synthetic method and an application of the platinum (II) complex. The platinum (II) complex takes 4'-(4-N,N-diethylamine phenyl)-2,2':6', 2''-terpyridyl as a ligand. The complex is obtained by dissolving a compound as shown in a formula (II) and dichloro.di(dimethyl sulfoxide)-platinum in a polar solvent and performing a complexing reaction; the complex can be synthesized through a solution method specifically, and can also be synthesized through a solvothermal method. An applicant investigates the proliferating inhibitory activity of the complex to multiple human tumor cell lines, and the results show that the complex has a remarkable antitumor activity in vitro, has good potential medicinal value and is expected to be used for the preparation of all kinds of antitumor drugs. The chemical structural formula of the complex provided by the invention is shown as the following formula (I).

The invention discloses a copper metal complex and a compound prepared from the copper metal complex and human serum albumin as well as a synthesis method and application thereof. The synthesis method of the copper metal complex comprises the following steps: taking phenyl-2-pyridyl ketone and 4,4'-dimethyl-3-thiosemicarbazide, taking an alcohol material as a solvent, reacting, generating precipitate, collecting the precipitate and washing the precipitate to obtain a ligand; taking the ligand which is phenyl-2-pyridyl ketone and contracting 4,4'-dimethyl-3-thiosemicarbazide and CuC12.2H2O, taking the alcohol material as the solvent, reacting, enabling a reactant to stand, crystallizing and collecting crystals to prepare the copper metal complex. The compound is prepared by incubating the copper metal complex and human serum albumin through a solution process. The structure of the copper metal complex is as shown in the following formula (I) which is as shown in the description.

The invention provides a skin moisturizer for treating a skin disease and a preparation method of the skin moisturizer. The skin moisturizer is mainly prepared from the following raw materials in parts by weight: 10-20 parts of alginate oligosaccharide, 0.5-5 parts of a solubilizer, 0.5-1 part of sodium chloride, 5-10 parts of a dispersing agent, 5-20 parts of a tackifier, 2-3 parts of a preservative and 2-3 parts of an antioxidant, wherein the solvent is injection water; and the preparation method comprises the following steps: dissolving 0.2-0.3 part of sodium chloride into residual injection water; adding the solubilizer, the tackifier, the preservative, the dispersing agent and the antioxidant, stirring evenly, and adjusting the pH value to be 3.5-6.5; dissolving the alginate oligosaccharide into the residual injection water, adding residual sodium chloride, stirring and mixing with the substances obtained from the steps; and packing and sterilizing to obtain the skin moisturizer. The skin moisturizer provided by the embodiment has the effects of good treatment effect, mild medicine property and no side effect.

The invention discloses a platinum complex for inhibiting cell SKOV3 and a synthesis method of the platinum complex, belongs to the technical field of medicines, and aims to provide a cell SKOV3 inhibiting platinum complex synthesized from rutaecarpine as structural basis and DMSO as an auxiliary ligand. The invention further provides a synthesis method of the platinum complex. The structural formula of the platinum complex is as shown in the description. The platinum complex can be used for preparing anti-tumor drugs.

The invention discloses a series of new 6-hydroxyloxoisoaporphine rare earth complexes, having a structural general formula as shown in specification, wherein Ln is La, Ce, Pr, Nd, Sm, Eu, Gd, Tb or Dy. The complexes are synthesized from 6-hydroxyloxoisoaporphine and the rare earth metal nitrates (Ln(NO3)3.xH2O as raw materials through a heating or reflux reaction. According to the complexes and the synthetic method and application thereof disclosed by the invention, the proliferation inhibition activity of the complexes to a plurality of human tumor cell strains such as SK-OV-3, SK-OV-3 / DDP and T-24 is investigated, and results indicate that all of the complexes have remarkable antitumor activity in vitro; in particular, the 6-hydroxyloxoisoaporphine lanthanum complex has extremely remarkable activity to cervical cancer cells SK-OV-3; in addition, apart from the 6-hydroxyloxoisoaporphine europium complex, the other complexes all have a good inhibition effect on human ovarian cancer / cis-platinum persisters SK-OV-3 / DDP.

The invention discloses coumarinolignoid and a preparation method and application thereof. The coumarinolignoid specifically comprises six compounds obtained through separation of Sapium discolor (Champ.ex Benth.)Muell.Arg.). Experiments show that the compounds can remarkably inhibit NO release of BV2 microglial cells stimulated by LPS under the condition that the survival rate of the BV2 microglial cells is not influenced by the compounds. The inhibitory effect of the compound 2a is slightly stronger than that of clinically common medicine, namely minocyline, and the compounds are good in potential medicinal value and are expected to be used for preparing medicines for neurodegenerative diseases.

The invention discloses an acridine-1, 3, 4-thiadiazole type compound and a preparation method and application thereof. The preparation method of the acridine-1, 3, 4-thiadiazole type compound comprises the following steps: 1) reacting by taking o-bromobenzoic acid and p-methyl aniline as raw materials, taking potassium carbonate and copper powder as catalysts and taking isoamyl alcohol or n-amyl alcohol as a solvent to obtain a compound 1; 2) cyclizing the compound 1 with phosphorus oxychloride to prepare a compound 2; 3) dissolving the compound 2 in an organic solvent, and then reacting with sodium thiocyanate in the presence of tetrabutyl ammonium bromide to prepare a compound 3; 4) taking the compound 3, dissolving in the organic solvent, and reacting with p-methoxybenzhydrazide to prepare a compound 4; and 5) taking the compound 4, reacting with concentrated sulfuric acid or acetic acid, adding water into a reactant to precipitate solids, and performing suction filtration for preparation. In-vitro anti-tumor test results show that the acridine-1, 3, 4-thiadiazole type compound has significant in-vitro anti-tumor activity against four subjects, namely MGC80-3, BEL-7404, NCI-H460 and T24.

The invention discloses a 3-benzimidazole-2(1H)-quinolinone derivative and a preparation method and application thereof. The preparation method of the derivative includes: dissolving a 2(1H)-quinolinone derivative and an o-phenylenediamine derivative in an organic solvent, and reacting under the condition of heating to obtain the 3-benzimidazole-2(1H)-quinolinone derivative. Compared with common antitumor drug 5-FU and cisplatin, the derivative has the advantages that some derivatives in the derivative have more efficient activity, and have low toxicity on normal hepatocytes HL-7702. The 3-benzimidazole-2(1H)-quinolinone derivative is shown as in the following structural formula, wherein R1 is hydrogen, methyl and methoxyl, or forms 1,2-methylenedioxy with R2; R2 is hydrogen, or forms 1,2-methylenedioxy with the R1; R3 is hydrogen, methyl, methoxyl, fluoro, chloro, bromo, nitro or trifluoromethyl; R4 is hydrogen, methyl, methoxyl or chloro.

The invention discloses a rare earth chelate compound with oxidized glaucine as a ligand. The structural formula of the rare earth chelate compound is shown as a formula (I), wherein M represents one tervalent rare earth cation ion in a period table of elements, and L represents an anion of rare earth metal salt when the rare earth cation participates in reaction in a form of the metal salt, namely, L represents nitrate radical or acetate radical. The rare earth chelate compound with oxidized glaucine as a ligand is synthesized by using a normal pressure solution method or high pressure solvent thermal method. The invention also discloses an inhibition effect of the rare earth chelate compound on various tumor cell strains. Results indicate that multiple rare earth chelate compounds show stronger antitumor activities as compared with the oxidized glaucine ligand, thus the rare earth chelate compound disclosed by the invention has a good potential medicinal value and is hopefully used for preparation of various antitumor medicaments.

The invention discloses a series of metal complexes of quinolinone derivatives, a synthesis method, and applications thereof. The synthesis method comprises the following steps: weighing metal salts and ligand 3-(1H-benzimidazole-2-yl)-6-methyl-2(1H)-quinolinone according to the stoichiometric ratio, dissolving the metal salts and ligand in a polar solvent, and carrying out coordination reactions to obtain the target products. The applicant also investigates the proliferation inhibition activity of the complexes on 4 human tumor cell strains and 1 normal cell strains. The results show that the complexes have a certain in-vitro antitumor activity; the activity of Rh(III) complexes is the most prominent, the antitumor activity of Rh(III) complexes on stomach cancer cell (MGC-803) is 5 times stronger than that of cis-platinum, furthermore, the toxicity of the complexes on the normal cells is smaller than the toxicity on cancer cells, the potential pharmaceutical value of the complexes is high, and the complexes are advantageously applied to the preparation of various antitumor drugs. The structure of the quinolinone metal complexes is shown in the description.

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.

The invention discloses a series of rhein aminophosphonate derivatives, and a synthetic method and applications thereof. The synthetic method of the rhein aminophosphonate derivatives comprises: taking rhein and an alpha-aminophosphonate as raw materials, dissolving in a polar solvent, in the presence of a catalyst HOBT and a condensing agent EDAC, reacting completely; and adding trichloromethane into the reaction liquid, washing with water, collecting the organic layer, applying to silica gel for column chromatography, eluting with a mixed solvent of ethyl acetate and petroleum ether with a volume ratio of 1:4-100 to obtain the corresponding derivative. The rhein aminophosphonate derivatives have the structural general formula (I) as shown in the description, wherein R is p-bromophenyl, o-bromophenyl, m-bromophenyl, p-fluorophenyl, o-fluorophenyl, p-chlorophenyl, m-chlorophenyl, o-chlorophenyl, m-methoxyphenyl, o-methoxyphenyl, phenyl, naphthyl, p-methoxyphenyl, m-methylphenyl, p-methylphenyl, m-fluorophenyl or anthryl.

The invention discloses a copper metal complex and a compound of copper metal complex and human serum albumin, as well as synthesis methods and application of the copper metal complex and the compound. The synthesis method for the copper metal complex comprises the following steps of reacting 2-di-pyridyl ketone with 4,4minute-dimethyl-3-thiosemicarbazide to generate precipitates by taking an alcohol substance as a solvent, and collecting and washing the precipitates to obtain ligands; reacting the ligands with CuCl2.2H2O by taking an alcohol substance as a solvent, standing and crystallizing a reaction product, and collecting crystals to obtain the copper metal complex. The compound is obtained by incubating the copper metal complex and the human serum albumin by adopting a solution method. The structure of the copper metal complex is shown in Formula (I).

The invention discloses a 5-bromo oxoisoaporphine, and a synthesis method and application thereof. The synthesis route of the 5-bromo oxoisoaporphine comprises the following steps: reducing 4-bromobenzylcyanide used as an initial raw material to obtain 4-bromobenzylethylamine, reacting the 4-bromobenzylethylamine with phthalic anhydride, and performing Friedel-Crafts acylation cyclization reaction twice, thus obtaining the 5-bromo oxoisoaporphine through synthesis. The applicant surveys the proliferation inhibition activity of the 5-bromo oxoisoaporphine on multiple human tumor cell strains, and results show that the 5-bromo oxoisoaporphine has remarkable in-vitro antitumor activity, has good potential pharmaceutical values and is hopefully used for the preparation of various antitumor medicaments. The chemical structural formula of the 5-bromo oxoisoaporphine is shown as below in the specification.

The invention discloses a 2-phenylpyridine dual-core palladium (II) complex. The structural formula of the complex can be seen in the description. The invention further discloses a preparing method ofthe 2-phenylpyridine dual-core palladium (II) complex. The method includes the steps of evenly mixing glacial acetic acid, palladium acetate and 2-phenylpyridine, conducting complete reaction under stirring and heating, conducting cooling to the room temperature, removing glacial acetic acid to obtain reddish brown liquid, adding a polarity solvent, and conducting standing until yellow crystals are separated out thoroughly to obtain the 2-phenylpyridine dual-core palladium (II) complex. The invention further discloses application of the 2-phenylpyridine dual-core palladium (II) complex. The 2-phenylpyridine dual-core palladium (II) complex has remarkable in-vitro antineoplastic activity and cytotoxicity selectivity and is simple in preparing method and easy to industrially produce.

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.

The invention discloses a copper (II) chloride chelate using 1-pyridyl-beta-carboline as a ligand and a synthetic method and application thereof. The structural formula of the copper (II) chloride chelate is shown as a formula (I). The preparation method of the chelate comprises the following steps that a compound shown in a formula (II) and copper chloride dihydrate are dissolved in a polar solvent to conduct a coordination reaction, and the copper (II) chloride chelate is obtained. The copper (II) chloride chelate performs an anti-tumor activity stronger than the anti-tumor activity of the ligand and cisplatin and has good potential medicinal value, and the copper (II) chloride chelate is expected to be used for preparing various anti-tumor medicines. Please see the structural formula (I) and the formula (II) in the specifications.

The invention discloses a metal complex taking oxidized nantenine as a ligand and a synthetic method and applications thereof. The metal complex is prepared by carrying out a coordination reaction on oxidized nantenine as the ligand and metal chloride in a polar solvent. Results obtained by investigating the proliferation inhibition effect of the metal complex on various tumor cell strains by the applicant show that the metal complex has an antitumor activity stronger than that of an oxidized nantenine ligand, and the antitumor activity of metal complex to part of tumor strains is obviously better than that of a clinical antitumor drug cis-platinum, therefore, the metal complex has a good potential medicinal value, and is expected to be used for preparing various antitumor drugs. The structure of the metal complex is shown in the specification, wherein M refers to a metal element selected from the fourth or fifth period in periodic table of elements, and X refers to water (H2O), dimethyl sulfoxide (DMSO), chlorine (Cl) or dehydrogenated methanol.

The invention relates to a beta-carboline compound and a synthetic method and application thereof, and belongs to the technical field of medicine. The structure of the compound is shown as the formula I (the formula I is shown in the specification). After an initial test, it is indicated that the in-vitro anti-renal-fibrosis activity of the compound is remarkable, the treatment effect on renal interstitial fibrosis caused by obstruction of the left ureter of a Balb / c mouse is good, the good potential medical value is achieved, and the beta-carboline compound and the synthetic method and application thereof can be used for preparing various kinds of anti-renal-fibrosis and anti-chronic-kidney-disease medicine.

The invention discloses two novel ruthenium and rhodium metal complexes taking lysicamine as ligands as well as a synthetic method and application of the two novel ruthenium and rhodium metal complexes. The synthetic method of the ruthenium and rhodium metal complexes comprises the following steps: dissolving dichloro.tetra(dimethyl sulfoxide) ruthenium (II) or rhodium trichloride and lysicamine into a polar solvent, and performing complexation reaction to prepare the ruthenium and rhodium metal complexes, wherein the ruthenium and rhodium metal complexes can be synthesized by virtue of solution methods or solvothermal methods. After the applicants investigate the proliferation inhibition activity of the ruthenium and rhodium metal complexes on human tumor cell lines such as NCI-H460, HepG-2, DLD-1 and MGC80-3 and the toxicity of the ruthenium and rhodium metal complexes to human normal liver cells HL-7702, results show that the ruthenium and rhodium metal complexes have significant in-vitro anti-tumor activity, and the activity of a rhodium metal complex is equal to that of cis-platinum; moreover, the ruthenium and rhodium metal complexes have relatively low cytotoxicity to normal cells, have good potential medicinal values, and are expected to be applied to the preparation of various anti-tumor medicines; and structural formulas of the complexes are respectively shown in the following formula (I) and formula (II) in the specification.

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.

The invention discloses a platinum (II) complex by taking chiral 4-(2,3-dyhydroxylpropyl)-methanamide-6-aza-benzanthrone as a ligand as well as a synthetic method and application of the platinum (II) complex. The synthetic method of the complex comprises the following steps: dissolving (+)-4-(2,3-dyhydroxylpropyl)-methanamide-6-aza-benzanthrone or (-)-4-(2,3-dyhydroxylpropyl)-methanamide-6-aza-benzanthrone and dichloro.bi(dimethyl sulfoxide)mixed platinum (II) in a polar solvent, mixing to carry out a complexing reaction, thereby obtaining the platinum (II) complex. The complex obtained by the inventor has obvious in-vitro antitumor activity, the in-vitro antitumor activity of a tested tumor strain is universally higher than that of an original chiral ligand, and the complex has high potential medicinal value and is expected to be used for preparing various antitumor medicines. The structural formulas of the complex disclosed by the invention are respectively shown in the formulas (I) and (II) in the specification.