1724 results about "Anti tumor drug" patented technology

Novel polymeric micelles which are used to deliver therapeutic agents, including anti tumor drugs.

The invention belongs to the field of medicine, and in particular relates to a medical application of 2-([1,1'-biphenyl]-4-yl)-2-oxoethyl 4-((3-chloro-4-methylphenyl) amino)-4-oxobutanoate in a selective histone lysine-specific demethylase 1 (LSD1) inhibitor, especially the application in anti-tumor medicaments. Pharmacodynamic tests indicate that the 2-([1,1'-biphenyl]-4-yl)-2-oxoethyl 4-((3-chloro-4-methylphenyl) amino)-4-oxobutanoate has a remarkable LSD1 inhibiting effect, and has selectivity to homologous proteins MAO-A (monoamine oxidase-A) and MAO-B.

The invention discloses a cyclopropylfluoroquinolone C-3 s-triazole thioether ketone thiosemicarbazone compound and a preparation method and application thereof. The chemical general structure of the compound is shown in formula I, in which R is at least one of H, ether group, hydroxyl, methyl, halogeno-group and nitro. According to the cyclopropylfluoroquinolone C-3 s-triazole thioether ketone thiosemicarbazone compound disclosed by the invention, a fluoroquinolone framework is actively overlaid or structurally complemented with three different pharmacophores such as a s-triazole heterocyclic ring, thiosemicarbazone and the like, so that the anti-tumor activity of the novel compound is increased, the toxic and side effects of normal cells are reduced, and the compound can serve as an anti-tumor activity matter to develop an anti-tumor drug of a novel structure.

The invention relates to a hyaluronic acid-modified amphipathic chitosan derivative carrier with tumor microenvironment specificity drug release effect. The hyaluronic acid-modified amphipathic chitosan derivative carrier is characterized in that firstly, a hydrophilic group is introduced into a chitosan skeleton; then, a hydrophobic group is introduced into a specifically degradable link arm containing disulfide bonds, so as to realize the amphipathic function; the amphipathic derivative is assembled into nanomicelle by self in a waterborne medium, and is further modified by a charge adsorbing principle to target the molecular hyaluronic acid; the nanomicelle can effectively load an anti-tumor drug, and the hyaluronic acid is targeted to the tumor microstructure and then is degraded by hyaluronic acid enzyme in focus cells, so that the drug can be quickly released from the nanomicelle to act on the focal part, thereby obviously improving the concentration, therapy effect and biological utilization degree of free drug on the focal part. The hyaluronic acid-modified amphipathic chitosan derivative carrier has the advantages that the carrier which carries pharmaceutical activity or pharmacological activity molecules can be applied to internal injection of blood vessels or muscles or oral administration, so as to obviously improve the anti-tumor activity of drug; the preparation method is simple, the technology is matured, and the preparation method is suitable for large-scale production.

The invention discloses a pH-responsive anti-tumor drug carrier material and a preparation and application of the pH-responsive anti-tumor drug carrier material. The preparation method comprises the following steps that (1) gold nanoparticles wrapped by mesoporous silica are prepared, and the gold nanoparticles comprise gold nanospheres or gold nanorods; (2) gold nanoparticles wrapped by carboxylation mesoporous silica are prepared; (3) water-soluble zinc oxide quantum dots are prepared; and (4) the pH-responsive anti-tumor drug carrier material is prepared. According to the pH-responsive anti-tumor drug carrier material and the preparation and application of the pH-responsive anti-tumor drug carrier material, the whole technological process design of the preparation method, the parameter conditions adopted by the reaction steps and the like are optimized, and the existing problems that drug releasing is uncontrollable, the drug loading capacity is low, and side effects are prone to being caused when the gold nanoparticles wrapped by the mesoporous silica serve as a drug carrier can be effectively solved.

The invention relates to theanine-modified carboline acyl amino acid benzyl ester, as well as preparation, anti-tumor activity and application thereof, discloses 17 compounds represented by a general formula I (in the formula, AA is selected from L-Leu, L-Glu, L- Val, L-Trp, L-Pro, L-Tyr, L-Met, L-Phe, L-Ala, L-Gly, L-Asn, L-Asp, L-Ile, L-Lys, L-Ser and L-Theanine residues, or AA-OBzl jointly represents OBzl), and discloses preparation and synthesis methods thereof. The invention further discloses in-vivo and in-vitro anti-tumor activity thereof and clinical application prospects thereof as anti-tumor medicaments.

The invention discloses a type of amino acid modified curcumin, a synthesis method thereof, and an application thereof. According to the invention, structural modification is carried out upon curcumin by using natural amino acid, such that 1-(4-hydroxy-3-methoxyphenyl)-7-(4-oxyacetyl amino carbobenzoxy-3-methoxyphenyl)-1,6-heptadiene-3,5-diketone which is represented by a general formula (I) is obtained. With an MTT method, evaluation is carried out upon the compound represented by the general formula (I) in the inhabitance of proliferation activities of four cells which are K562, H22, HL60 and S180. IC50 values of the compound represented by the general formula (I) in inhibiting the proliferations of the four tumor cells are calculated. As a result of experiments, with the compound represented by the general formula (I), proliferations of tumor cells can be substantially inhibited. The compound has excellent anti-tumor activity, and can be prepared into anti-tumor medicines.

The invention discloses substituted-evodiamine anti-tumor and antifungal compounds and a preparation method thereof. The compounds have a general structural formula (I), wherein R represents: (1) benzyl or substituted benzyl; (2) benzoyl or substituted benzoyl; (3) linear or branched alkyl having 2 to 6 carbon atoms; and (4) an ester group. The substituted-evodiamine compounds of the invention have good anti-tumor activities for various tumor cells, provide a new way for deep research and development of new anti-tumor medicaments and can be used for preparing new anti-tumor medicaments.

The invention provides a method for preparing an anti-tumor T cell in vitro through DC (dendritic cell, namely antigen presenting cell), wherein the anti-tumor T cell is a tumor total RNA-loaded DC amplification and enrichment anti-tumor T cell. The invention also provides a preparation method of the anti-tumor T cell and an anti-tumor drug or inoculation vaccine taking the anti-tumor T cell as an active ingredient. According to the invention, a specific anti-tumor T cell is amplified in vitro by taking the tumor total RNA-loaded DC as a platform, a small amount of tumor total RNA is amplified to an enough amount in vitro so as to realize clinical application, and the in-vivo anti-tumor effect in an IC (intracranial) tumor-bearing model is evaluated, including how the mature state of DC and the cell factor combination adjust the differentiation of the anti-tumor T cell as well as the synergistic anti-tumor effect thereof in a preclinical experiment model.

The present invention relates to a pentacyclic triterpanoid derivative of multiple-oxide substitution of the A ring and the medicine salt or solvate of the derivative, and the present invention also relates to the preparation method, the drug combination, and medical use of the derivative. The compound of the present invention has the functions of inhibiting the activity of six human tumor cell strains in vitro, such as human prostate cancer cell (PC-3), nasopharyngeal carcinoma cells (CNE), oral squamous carcinoma cell(KB), human lung cancer cell (A549), human hepatoma cell (BEL-7404), and human cervix cancer cell (Hela), and the function of the invention is at the same magnitude of the positive control of cisplatin, thereby the compound can be used as expected antitumor drug. The compound of the present invention also inhibits the alpha glucosidase strongly, and the inhibiting effect is greater than the positive control of acarbose, thereby the compound can be used as expected medicine for preventing and treating diabetes and the treatment of the virus diseases.

The invention relates to the technical field of medicines and in particular relates to oxa- or thio-evodiamine anti-tumor derivatives as well as a preparation method of the derivatives and application of the derivatives in preparation of topoisomerase inhibitors and anti-tumor drugs. The oxa- or thio-evodiamine anti-tumor derivatives are newly discovered topoisomerase I inhibitors with brand-new structures and have remarkable anti-tumor activity, and the structure of a compound is as shown in a general formula I.

The invention discloses conjugates of beta-carboline-3-carboxylic acid and oligopeptides, preparation, a nano structure, and an application thereof as an antitumor agent. The invention discloses conjugates (8a-f) of beta-carboline-3-carboxylic acid and six oligopeptides, wherein the six oligopeptides are Leu-Pro-Asn-Ile-Ser-Lys-Pro (LPNISKP), Arg-Gly-Asp-Ser (RGDS), Arg-Gly-Asp-Phe (RGDF), Arg-Gly-Asp-Val (RGDV), Leu-Asp-Ser (LDV), and Lys-Glu (KE). The invention discloses a preparation method and nano structure of the conjugates, discloses an inhibition effect of the conjugates on five tumor cell strains namely HL60, HCT-8, HeLa, BEL-7402, and HepG2, and further discloses an inhibition effect on tumor growth of S180 tumor-bearing mice. The experiment results show that the provided conjugates of beta-carboline-3-carboxylic acid and six oligopeptides have an excellent antitumor effect, so that the conjugates is advantageous for being used as an antitumor drug in clinic.

The invention discloses application of fructus forsythiae aglycone in preparing a medicament for preventing or treating liver injury or liver failure, and belongs to the medical field. The fructus forsythiae aglycone is a traditional Chinese medicine monomer obtained by extracting from the conventional fructus forsythiae, and is shown to have better treatment effect for the liver injury caused by acetaminopben, the livery injury caused by anti-tumor drug cis-platinum, acute or chronic livery injury caused by carbon tetrachloride, the livery injury caused by D-galactosamine and the liver failure caused by the D-galactosamine and lipopolysaccharide according to an animal test, has effect, which is better than that of fructus forsythiae and fructus forsythiae aglycone, in treating liver injury or liver failure. The fructus forsythiae aglycone is exact in curative effect and low in side effect for treating the liver injury and the liver failure, and has wide medical application prospect.

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 belongs to the field of medicinal chemistry and discloses pyrimidotriazole compounds containing hydrazine bonds as well as a preparation method and an application of the pyrimidotriazole compounds in drug preparation. The general formula I of the compounds is shown in the specification. The compounds have remarkable inhibition and killing functions on multiple tumor cells such as MGC-803, MCF-7 and EC-109, can serve as candidate or lead compounds for further development and are applied to preparation of an anti-tumor drug.

The invention relates to the field of natural drug and medicinal chemistry, in particular to ursane-type pentacyclic triterpenoid amino acid derivatives (I), and the preparation method and the medicinal application thereof. The compounds have effect on inhibiting glycogen phosphorylase, and can be used for preparing drugs for resisting diabetes, cerebral ischemia, cardiovascular diseases, hyperlipemia, obesity, atherosclerosis and tumor. The invention also relates to the preparation method of the compounds and drug preparations containing the compounds.

The invention belongs to the fields of supramolecular polymer polymer chemistry and drop formation control, and particularly relates to supramolecular hydrogel microsphere modified with cyclodextrin water-solubility polymer and adamantine water-solubility polymer and formed by assembling subjective and objective bodies in a liquid drop, and a preparation method and application thereof. The first purpose of the invention is to provide novel supramolecular hydrogel microsphere formed by assembling subjective and objective bodies and a preparation method thereof method, the second purpose of the invention is to adopt liquid drop as a template to realize supramolecular assembly and achieve uniform particle size and controllable dimension of the supramolecular hydrogel microsphere, and the third purpose of the invention is to provide application of the type of supramolecular hydrogel microsphere in adriacin doxorubicin and taxol water-solubility antitumor drug sustained release, so as to achieve the purpose that a drug can keep a high concentration level for a long time.

The invention relates to a tumor inhibitory peptide capable of being specifically bound with PD-1 and an application thereof. The inhibitory peptide can be bound with an extracellular region of a PD-1 protein receptor and can effectively close a PD-1 protein at protein level and cellular level and prevent the PD-1 protein from being bound with a ligand PD-L1. The polypeptide has good biological activity. The polypeptide can be used in tumor immunotherapy alone or combined with an anti-PD-1 monoclonal antibody or other anti-tumor drugs as well as diagnosis and screening of a PD-1 positive tumor patient, namely the polypeptide can be applied to preparation of drugs used for treating tumor and autoimmune diseases.

The invention relates to a preparation method of a water-soluble magnetic targeting graphene oxide derivative and an application thereof. The problems of low curative effect and large side effects in the prior art can be effectively solved. The technical scheme for solving the problems is as follows: loading magnetic ferroferric oxide on graphene oxide through a chemical precipitation method, and then connecting with a hydrophilic group to get the water-soluble magnetic targeting graphene oxide derivative. In the graphene oxide derivative, the weight ratio of the ferroferric oxide to the graphene oxide is 1-11:1; and the graphene oxide is nano-scale graphene oxide. The water-soluble magnetic targeting graphene oxide derivative disclosed by the invention has the advantages of good physical and chemical stability, rich sources of raw materials, low cost, good biocompatibility, slow release and targeting property, and is of an innovation in anti-tumor medicaments.

This invention relates to a method for preparing immunogen G17CRM197 containing diphtherin mutant CRM197 as carrier. The method comprises: crosslinking diphtherin mutant CRM197 with gastrin G17 through epsiv-maleimidyl caproic acid N-hydroxysuccinimide eater (EMCS). Diphtherin mutant CRM197 is used as a carrier, and has such advantages as high recovery rate and easy purification. The method has such advantages as high product crosslinking rate, short preparation time, and low cost. Immunogen G17CRM197 can be used as an effective component in therapeutic vaccines, or used in anti-tumor drugs with appropriate immunoadjuvants.