1769 results about "Anti tumor drug" patented technology

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

The invention discloses a pyrimidoheterocyclic compound represented as the formula (I), or a pharmaceutically acceptable salt or a stereisomer thereof, or a prodrug molecule thereof. The pyrimidoheterocyclic compound can effectively inhibit growth of various tumor cells and has an inhibiting effect on EGFR protease. The pyrimidoheterocyclic compound can be used for preparing an anti-tumor drug, and can overcome drug resistance caused by medicines in the prior art, such as gefitinib, erlotinib and the like, has a selectivity on wild non-small cell lung cancer and is excellent in pharmacokinetic property.

The invention relates to an amphiphilic block copolymer and a preparation method thereof, and a micelle drug delivery system formed by the copolymer and an anti-tumor drug. The amphiphilic block copolymer comprises a hydrophilic chain segment and a hydrophobic chain segment, and the end of the hydrophobic chain segment is sealed by hydrophobic radicals. According to the amphiphilic block copolymer disclosed by the invention, methoxy polyethylene glycol (or polyethylene glycol)-polyester segmented copolymer with generally recognized safety is taken as a base material, and terminated hydroxyl hydrophobic radicals of the polyester chain segment are modified, thus the compatibility of hydrophobic chain segments in drug molecules and segmented copolymers is improved, and mutual acting force is increased; through a self-assembling method, the drug can be solubilized in micelle hydrophobic cores of the amphiphilic block copolymer, and the drug molecules are limited in the micelle cores so as not to be likely to be dissolved out, thus drug delivery micelle with high stability is obtained.

The present invention provides a cobalamin-drug conjugate suitable for the treatment of tumor related diseases. Cobalamin is indirectly covalently bound to an anti-tumor drug via a cleavable linker and one or more optional spacers. Cobalamin is covalently bound to a first spacer or the cleavable linker via the 5′-OH of the cobalamin ribose ring. The drug is bound to a second spacer of the cleavable linker via an existing or added functional group on the drug. After administration, the conjugate forms a complex with transcobalamin (any of its isoforms). The complex then binds to a receptor on a cell membrane and is taken up into the cell. Once in the cell, an intracellular enzyme cleaves the conjugate thereby releasing the drug. Depending upon the structure of the conjugate, a particular class or type of intracellular enzyme affects the cleavage. Due to the high demand for cobalamin in growing cells, tumor cells typically take up a higher percentage of the conjugate than do normal non-growing cells. The conjugate of the invention advantageously provides a reduced systemic toxicity and enhanced efficacy as compared to a corresponding free drug.

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 provides a sustained-release temperature-sensitive blood vessel embolic gel used for treating tumor. The sustained-release blood vessel embolic gel is prepared by entrapping a medicine by using a pharmaceutically acceptable carrier. The medicine is an anti-tumor medicine, and the pharmaceutically acceptable carrier comprises a gel prepared from poloxamer polymer, polyvinyl pyrrolidone, and the like or a composition thereof. The polymer material accounts for 5-65% of a gel mass. The particle size of the gel is in a range of 10nm to 150mum. The embolic agent is liquid gel under normal temperature, and can be used for direct injection through catheter. After injection into body, with the increase of temperature, the liquid gel is rapidly solidified into gel. Also, according to requirements, different medicines can be entrapped, and embolism and medication dual effect can be achieved through local sustained-release. Therefore, the gel provided by the invention can be used as an embolic agent for endovascular treatment, and can be used in various benign and malignant tumor transcatheter arterial chemoembolizations. The preparation method provided by the invention is simple, and is suitable for industrialized productions.

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 belongs to a liposome, in particular relates to a compound liposome preparation with high targeting property of tumor tissues and efficient penetrability of tumor cells. The invention is characterized in that hyaluronic acid or sodium hyaluronate, tumor cell selective penetrating peptides and a liposome are used for together constructing a compound liposome. The compound liposome is characterized by utilizing the dual-tumor cell targeting property of the hyaluronic acid and tumor cell selective penetrating peptides to effectively solve the problem that because a conventional liposome and traditional cell penetrating peptides have no selectivity on normal cells and tumor cells, the toxicity is increased when the drug effect is increased in the therapeutic process, thereby fully meeting the clinical requirements of high efficiency and low toxicity when anti-tumor drugs are prepared into preparations for treating diseases.

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 discloses a pyrimidoheterocyclic compound represented as the formula (I), or a pharmaceutically acceptable salt or a stereisomer thereof, or a prodrug molecule thereof. The pyrimidoheterocyclic compound can effectively inhibit growth of various tumor cells and has an inhibiting effect on EGFR protease. The pyrimidoheterocyclic compound can be used for preparing an anti-tumor drug, and can overcome drug resistance caused by medicines in the prior art, such as gefitinib, erlotinib and the like, has a selectivity on wild non-small cell lung cancer and is excellent in pharmacokinetic property.

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 invention discloses 14 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters shown in the general formula I. In the general formula I, AA represents L-Ser residue, L-Glu (OBzl) residue, L-Phe residue, L-Val residue, L-Arg residue, L-Tyr residue, L-Ala residue, L-Trp residue, L-Asn residue, L-Met residue, L-Ile residue, Gly residue, L-Asp (OBzl) residue or L-Leu residue. The invention discloses a preparation method of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, discloses HT-29, K562, A549 and HL60 tumor cell growth inhibition effects of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, further discloses S180-loading mice tumor growth inhibition effects of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters, and also discloses use of the 3H-imidazo[4,5-c]pyridine-6-formyl-amido acid benzyl esters as antitumor drugs.

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 relates to novel anti-tumor application of an alkaloid compound penicillium enol A1 from penicillium citrinum. The penicillium citrinum IBPT-5 is collected in the China Center for Type Culture Collection (CCTCC), which is located in Wuhan University and has the collection number of CCTCC NO:M2013713, on December 25, 2013. Experiments prove that the compound has better anti-tumor activity on various tumor cells, and can be used for preparing cell proliferation inhibition medicines or anti-tumor medicines for anti-tumor study, wherein tumor cells comprise human colon cancer cells SW620, human hepatoma cells Huh7, human gastric carcinoma cells BGC-823, human colon cancer cells SW480, human esophageal squamous carcinoma cells KYSE450, human esophageal cancer cells EC9706, human highly metastatic lung carcinoma cells 95-D, human hepatoma cells PLC and human gastric carcinoma cells HGC-27.

The invention specifically discloses a monoclonal antibody against human PD-1, and a preparation method and application thereof, belonging to the field of antibodies. The monoclonal antibody against human PD-1 in the invention has good biological activity, and can effectively bind to the extracellular region of a human PD-1 protein receptor, block PD-1 protein at a protein level and a cellular level, prevent binding of the PD- 1 protein to ligand PD-L1 and enhances immunity. The monoclonal antibody can be individually used or used in combination with other anti-tumor drugs for tumor immunotherapy and the diagnosis and screening of patients with PD-L1 positive tumors, and has good prospects in preparation of drugs for treating tumors, anti-autoimmune diseases and the like.

A 3-methoxy-flavone compound comprises 5,7-dihydroxy-8-(3,3-dimethyl diallyl)-3,3', 4'-trimethoxy flavone and 5, 7-2 dihydroxy-8- (3,3-dimethyl allyl)-3,4'-dimethoxy flavonoe. harmacological test results prove that: the 3-methoxy-flavone compound is an effective fatty acid synthase inhibitor, which shows the broad-spectrum anti-tumor effect in the cytotoxicity tests of various tumor cell lines and has strong tumor growth inhibiting effect on human prostate cancer cell LnCAP, human breast cancer cell ZR-75-1, human lung cancer cell NCI-H23 or human colon cancer cell HCT-116 when applied to human tumor transplant nude mice model tests. In addition, the 3-methoxy-flavone compound reveals no toxicity in mice acute toxicity tests, which then can be used as anti-tumor drug and is a new broad-spectrum anti-tumor drug with great development prospects.

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 preparation method and a drug carrying method of an escherichia coli outer membrane vesicle, and application of the outer membrane vesicle in anti-tumor. The preparation method of the escherichia coli outer membrane vesicle comprises the following steps of culturing a culture medium using LB in vitro, culturing an escherichia coli BL21 strain, performing centrifugation, filtration and ultrafiltration treatment to obtain an upper layer culture solution free of escherichia coli, and finally centrifuging the upper layer culture solution by a supercentrifuge to prepare the escherichia coli outer membrane vesicle. The particle size of the prepared escherichia coli outer membrane vesicle is uniform, and is about 50nm. Usually, a bacterium outer membrane vesicle is low in yield and difficult in drug carrying. The invention excogitates a novel drug carrying method for the bacterium outer membrane vesicle, so that the carrying efficiency of an anti-tumor drug can be significantly improved; an inhibition effect on multiplication and invasion of a tumor cell is increased; and a good application prospect of the bacterium outer membrane vesicle serving as a novel non-virus drug carrier is presented.

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.

With the current invention, we provide new methods of enhancing the T-cell stimulatory capacity of human dendritic cells (DCs) and their use in cancer vaccination. The method comprises the introduction of different molecular adjuvants to human DCs through transfection with at least two mRNA or DNA molecules encoding markers selected from the group of: CD40L, CD70, constitutively active TLR4 (caTLR4), IL-12p70, EL-selectin, CCR7 and / or 4-1 BBL; or in combination with inhibition of SOCS, A20, PD-L1 and / or STAT3 expression, for example through siRNA transfection. We could show a clear increase in the immunostimulatory capacity of DCs obtained in this way, enabling them to elicit an unexpectedly high T-cell immune response in vitro. Introduction of at least two of the above molecules, in combination with a tumor-specific antigen enables the DCs to elicit a significant host-mediated T-cell immune response in vivo against the tumor antigen and thus makes them very attractive in the manufacturing of anti-cancer vaccines.

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 present invention provides a therapeutic combination comprising (a) a compound of formula (I) as set forth in the specification and (b) one or more antineoplastic agents selected from the group consisting of an alkylating or alkylating-like agent, an antimetabolite agent, a topoisomerase I inhibitor, a topoisomerase 11 inhibitor, an inhibitor of a growth factor or of a growth factor receptor, an antimitotic agent, a proteasome inhibitor, an inhibitor of an anti-apoptotic protein and an antibody directed against a cell surface protein, wherein the active ingredients are present in each case in lice form or in the form of a pharmaceutically acceptable salt or any hydrate thereof.

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 provides a bufadienolides extraction extracted from the toad skin or the toad venom; wherein, the weight percentage of the bufadienolides (accounted by the cinobufagin) can reach above 55%. The invention adopts the extraction method that: the toad venom, the toad skin or the bufo siccus is extracted by the ethanol; after the recovery of the ethanol, the macroporous resin column on the concentration liquid is eluted by the water and the low concentration alcohol, and is eluted by the high concentration alcohol, then the final product is gained through collecting the eluent and reducing the pressure of the recovery solvent to pass drying or extraction. The invention has an advantage that: the invention also provides the drug composition using the extraction as the active component, the suppressing the tumour cells active function of the extraction and the application in the preparation of the anti-tumor drug.