129results about How to "Strong in vitro antitumor activity" patented technology

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 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.

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.

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.

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 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.

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.

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.

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 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.

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.

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.

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.

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.

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).