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 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 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 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 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 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.