1609 results about "Antitumor activity" patented technology

The invention belongs to the technical field of medicines, and particularly relates to quinazoline stilbene derivatives as well as a preparation method, a composition and application thereof. The quinazoline stilbene derivative is synthesized by combining quinazoline with pharmacophores such as a styrene skeleton, and the quinazoline stilbene derivative structurally contains functional units such as a quinazoline functional unit and the pharmacophores such as the styrene skeleton, so that the compound is endowed with good anti-tumor activity. Researches show that the quinazoline stilbene derivative has a good anti-tumor effect including KRASG12C mutation non-small cell lung cancer, has the advantage of multi-target action, has an adjusting effect on Src kinase and related downstream signal channels of Statat, mTOR, Akt and PI3k, and is beneficial to reduction of tumor drug resistance. Compared with a complex structure modified compound, the quinazoline stilbene derivative disclosed by the invention is simple in structure and easy to prepare, and has a good application prospect.

The invention relates to the field of natural products, in particular to a dimer compound of guaiane type sesquiterpenes and uric acid as well as an extraction and separation method and application of the dimer compound. According to the invention, a new dimer compound of guaiane type sesquiterpene and uric acid is extracted and separated from carpesium abrotanoides in Guizhou, and it is found that the dimer compound has relatively strong anti-tumor activity. The compound has strong inhibitory activity on breast cancer, prostate cancer, nasopharynx cancer, liver cancer, lung cancer, leukemia, pancreatic cancer, glioma, osteosarcoma, skin cancer, cervical cancer, ovarian cancer, kidney cancer and esophageal cancer, and provides an optional scheme for broad-spectrum anti-cancer drugs. Moreover, in human prostate cancer cells PC3, human cervical cancer cells Hela, human liver cancer cells HepG2 and human glioma cells U87 which are resistant to paclitaxel, the compound also shows strong anti-cancer activity, which indicates that the compound has the potential of treating patients resistant to paclitaxel.

The invention belongs to the technical field of biology, and provides a nanometer antibody targeting Nectin-4, and a nucleic acid molecule and an expression vector for coding the nanometer antibody targeting Nectin-4. The invention also provides a chimeric antigen receptor which comprises an extracellular antigen binding domain, a transmembrane domain and an intracellular domain, and the extracellular antigen binding domain is a Nectin-4 nano antibody; the invention also provides a chimeric antigen receptor CAR which contains the nano antibody as scFv and co-expresses CXCR1, a CAR-T cell constructed by the chimeric antigen receptor CAR, and an enhanced CAR-T cell obtained by modifying the CAR-T cell with microbial short-chain fatty acid, so as to improve the infiltration and anti-tumor activity of the CAR-T cell targeting Nectin-4.

The invention discloses application of camellia nitidissima exosome-like nano-vesicles in preparation of antitumor drugs, and belongs to the technical field of biological medicines. The exosome-like nano-vesicles are extracted from golden camellia for the first time, and the exosome-like nano-vesicles are proved to have remarkable anti-tumor activity.

The invention belongs to the technical field of medical materials, discloses hyaluronic acid modified phosphorus-doped double-copper monatomic nano-enzyme (Cu2 / PNC at HA) and a preparation method and application thereof, and aims to solve the problems of low catalytic efficiency and poor selectivity of nano-enzyme. The preparation method comprises the following steps: firstly synthesizing a ZIF-8 carrier, then coating double copper ions and poly (cyclotriphosphoryl-4 ', 4'-diaminodiphenyl ether) (PZM) on the surface of the ZIF-8 through polymerization, and further performing pyrolysis to obtain the Cu2 / PNC nano-enzyme. The catalytic efficiency of the Cu2 / PNC nano-enzyme is remarkably improved through the phosphorus doping effect and double copper single atoms. The hyaluronic acid is adopted to coat the Cu2 / PNC nano-enzyme, so that the biocompatibility is improved, the anti-tumor activity is remarkably improved, the application of the Cu2 / PNC nano-enzyme in the field of biomedicine is expanded, and the huge potential in the aspect of tumor catalytic treatment is shown.

The invention discloses a compound with anti-tumor activity. The compound has a chemical structural formula as shown in a formula (I). The compound belongs to a novel tetracyclic triterpenoid natural product, has good fat solubility and chemical stability, and can be conveniently extracted from the rhizome of a herbal medicine Polygala fallax Hemsl. And prepared into an oral or injection form. The invention also provides a preparation method and application of the compound. The compound provided by the invention can obviously inhibit the growth of mouse lung cancer and reduce the volume and weight of tumor, and can be used for treating tumor diseases.

The invention discloses erianin PROTACs as well as a preparation method and application thereof, the structural formula of the erianin PROTACs is # imgabs0 #, E3 Ligand is pomalidomide, and Linker is an alkane chain or a PEG chain. The erianin PROTACs disclosed by the invention are superior to the prior art in the aspects of target protein degradation efficiency, anti-tumor activity, innovativeness, application prospect and the like, and show remarkable technical progress and practical value.

The invention discloses a non-natural amino acid as well as a preparation method and application thereof. The novel non-natural amino acid is obtained by introducing long and soft side chain amino acid into a classical ASF side chain for the first time, the stability of the obtained non-natural amino acid is enhanced, the reaction radius of the non-natural amino acid is increased, the non-natural amino acid can touch amino acid residues with farther distance, and the reactivity is improved. In addition, compared with other covalent amino acids, the covalent amino acids have higher reaction rate and binding efficiency. The polypeptide and related drugs obtained based on the non-natural amino acid can be high in safety, can cross a blood brain barrier to realize brain targeting, and have better anti-tumor activity, so that the polypeptide and related drugs have extremely high medical value.

Provided herein are novel anti-CD20 x anti-CD28 antibodies and methods of using such antibodies for the treatment of B-cell malignancies. Subject anti-CD20 x anti-CD28 antibodies are capable of agonistically binding to CD28 costimulatory molecules on T cells and CD20 on tumor cells. Thus, such antibodies enhance anti-tumor activity at tumor sites. The subject antibodies provided herein are particularly useful in combination with other anti-cancer therapies (e.g., anti-CD3 x anti-CD20 x anti-CD79b antibodies) for the treatment of B-cell malignancies.

The present invention discloses a nano antibody against BCMA and its preparation method and application, and relates to the field of biomedical technology. The present invention uses CRISPR / Cas9 technology to knock out B2M and TRAC genes in T cells to prepare universal CAR-T cells; the nano antibody targeting BCMA and the natural ligand SIRPα extracellular N-terminal V region of CD47, the transmembrane region of CD28, the intracellular signal region of 4-1BB and the intracellular signal region of CD3ζ are connected in series to form a dual-targeted chimeric antigen receptor for the treatment of multiple myeloma, so as to solve the high recurrence problem faced by CAR-T cell therapy in the treatment of multiple myeloma. The universal CAR-T cells prepared by the present invention have strong killing activity against multiple myeloma cells, effectively improve the treatment effect, and provide a key material for the subsequent development of adoptive immunotherapy with high efficiency and lasting anti-tumor activity.

The invention discloses a multi-target anti-tumor active rutaecarpin derivative or a pharmaceutical salt thereof. The structural general formula of the rutaecarpin derivative or the pharmaceutical salt thereof is shown as a formula I or a formula II: # imgabs0 #, wherein R1 is selected from C1-C5 alkoxy, hydroxyl and hydrogen; r2 is selected from hydrogen and halogen; according to the present invention, the enzyme inhibition activity and in vitro anti-tumor activity test results show that the compound of the present invention has strong inhibition activity on topoisomerase 1, topoisomerase 2 and c-MYC oncogenes, such that the new approach is developed for the deep research and the development of the new structure type anti-tumor drug, and the new strategy is provided.

The present invention provides an antibody binding to human CD73, a preparation method therefor, and a use thereof. The monoclonal antibody of the present invention can bind to a CD73 antigen with high specificity, has high affinity, has remarkable anti-tumor activity and the like, and has excellent clinical application prospects.

The invention provides a gamma delta T cell preparation as well as a preparation method and application thereof, and belongs to the technical field of T cells. The liposome is prepared from the following raw materials in parts by weight: 15-20 parts of modified gamma delta T cell liposome, 1-3 parts of cell stimulating factors and 4-7 parts of culture medium freeze-dried powder, the modified gamma delta T cell lipidosome is prepared by embedding gamma delta T cells through lipidosome, coupling with acetylenic bond modified chitosan, and further mixing with MFAP4 protein and b4GALT1 protein. The culture medium freeze-dried powder is prepared by freeze-drying the culture medium in the engineering culture process of gamma delta T cells, and the cell stimulating factors are resveratrol and quercitrin. According to the gamma delta T cell preparation prepared by the invention, the survival ability and resistance of gamma delta T cells are improved, the anti-tumor activity of the gamma delta T cells is improved, and the gamma delta T cell preparation has relatively good antioxidant and anti-inflammatory effects, reduces the inhibition of inflammation on an immune system and has a very good treatment effect on pancreatic ductal adenocarcinoma.

The invention provides an AS01 derivative adjuvant, a preparation method thereof and application of the AS01 derivative adjuvant in preparation of vaccines or anti-tumor drugs, and belongs to the technical field of biological drugs or products. The AS01 derivative adjuvant is prepared from the following components in parts by mass: 0.5 to 1.0 part of cholesterol, 2.0 to 4.0 parts of dioleoyl lecithin and at least one of the following components in parts by mass: 0.1 to 0.2 part of monophosphoryl lipid A, 0.1 to 0.2 part of QS-21, 0.36 to 0.72 part of 3M-052, 0.4 to 0.8 part of muramyl dipeptide and 0.2 to 0.4 part of oligodeoxynucleotide. According to the AS01 derived adjuvant, a novel synergistic adjuvant system is developed by integrating various immunomodulators, so that the immunogenicity of a vaccine is enhanced. The HPV vaccine is prepared on the basis of the AS01 derived adjuvant, so that the immunogenicity can be enhanced, and good anti-tumor activity can be achieved. Therefore, the invention provides a new strategy for immunotherapy of HPV-related tumors.

The invention discloses an enantiokaurane compound with antitumor activity as well as a preparation method and application of the enantiokaurane compound. According to the present invention, chemical components of Western African plant I.trichantha tubers are deeply studied, and a variety of chromatographic separation methods such as macroporous resin, silica gel resin, medium pressure preparation-MCI column, gel normal pressure column and semi-preparative high performance liquid chromatography are combined to separate to obtain one enantiokaurane new compound Trichanthone B; experiments show that the compound obtained through separation has a good inhibition effect on an MIA PaCa-2 pancreatic cancer cell line and an A549 lung cancer cell line, and IC50 of the compound on the MIA PaCa-2 pancreatic cancer cell line reaches a nanomole level; the effect of the compound is stronger than that of positive drugs 5-fluorouracil and carboplatin, and the compound has the potential of being developed into new drugs for resisting pancreatic cancer and lung cancer.

The invention discloses an N-phenylbenzenesulfonamide compound as well as a preparation method and application thereof. The compound disclosed by the invention is shown as a formula (I). The compound is an LDHA enzyme inhibitor, is a sulfonamide compound with anti-tumor activity, shows good anti-tumor activity at the cellular level, has good safety and can be used for preparing anti-tumor drugs. # imgabs0 #

The invention discloses an anti-tumor matrine hydrazine thiazole derivative and a preparation method and application thereof.The preparation method comprises the steps that NaH is added into a first reaction container, then a DMF solution is added, thiosemicarbazide is added into the first reaction container, and the solution is stirred; adding sophocarpidine into the stirred solution to perform reflux reaction, performing quenching reaction after the reaction is finished, and performing extraction, concentration drying and column chromatography separation to obtain a thiosemicarbazide sophocarpidine intermediate; adding the obtained thiosemicarbazide matrine intermediate into a reaction container II, and adding a dissolving solvent ethanol for dissolving; adding alpha-bromo-R-ethyl ketone into the dissolved solution for reaction, concentrating and drying after the reaction is finished, and performing column chromatography separation to obtain the anti-tumor matrine hydrazine thiazole derivative. The anti-tumor matrine hydrazine thiazole derivative is high in anti-tumor activity, the preparation method is simple and convenient, and reaction conditions are easy to control.

The invention relates to a curcumin quantum dot, a preparation method thereof and application of the curcumin quantum dot in preparation of a tumor diagnosis and treatment integrated reagent. The curcumin quantum dot comprises a reaction product formed by performing a Schiff base reaction on curcumin and a polyamino ligand in the presence of a dehydrating agent, wherein the average diameter of the curcumin quantum dot is 1-30nm. The curcumin quantum dot provided by the invention can greatly improve the solubility, biocompatibility and antitumor activity of single curcumin.

The invention relates to a turtle-derived cyclic peptide compound with an anti-tumor effect and a preparation method thereof. The preparation method comprises the following steps: crushing tortoise plastron, adding water for reflux extraction, filtering, concentrating and drying to obtain tortoise-shell glue; dissolving the obtained tortoise-shell gelatin in water, adding protease for enzymolysis, and centrifuging after enzyme deactivation to take supernate; carrying out graded filtration on the obtained supernate and collecting components; and separating and purifying the collected components to obtain the cyclic peptide. The obtained compound has remarkable anti-tumor activity and has a good application prospect in preparation of anti-tumor drugs.

The invention discloses synthesis and antitumor activity research of a novel drug small molecular formula (1) containing a phenothiazine structure. R is # imgabs 1 #. 10H phenothiazine is used as an initial raw material, (E)-3-(10-ethyl-10H-phenothiazin-3-yl) acrylic acid is generated through a typical Friedel-Crafts alkylation reaction, an NBS bromination reaction and the like, and then an important intermediate compound 6 is synthesized through a Wittig reaction and a hydrolysis reaction. And carrying out coupling reaction on the intermediate compound 7 and different amine compounds to obtain 11 target compounds 7a-7k: formula (1). A CCK-8 experiment is carried out on a target compound to obtain a conclusion that the target compound 7a-7k and 5-fluorouracil are tested at the concentration of 20 mu M, and the result shows that the compound 7f has the best inhibition effect on A549, Hep G2 and HeLa cells, and the compound 7c has the better inhibition effect on the A549 cells. IC50 value calculation is carried out on a target compound under various concentrations, the IC50 value of 7c to HELA cells is small, the IC50 value of 7f to Hep G2 and HeLa cells is minimum, and the inhibition effect is the best. Therefore, the compound can be used for antitumor drugs.

The invention discloses an anti-tumor medicine composition combined with a PARG inhibitor and application. Through natural product library screening and CCK-8 experiments, it is found that PARG knockout gastric cancer cells show significantly enhanced sensitivity to ginsenoside CK. Further clone formation experimental analysis shows that PARG knockout significantly enhances the inhibitory effect of ginsenoside CK on gastric cancer cell proliferation. In in-vivo experiments, a CDX model is utilized to verify that PARG knockout can significantly enhance the anti-tumor activity of ginsenoside CK on gastric cancer. The discovery provides an important experimental basis for clinical application of PARG as a gastric cancer treatment target and ginsenoside CK as a potential treatment drug. The research finds that the PARG inhibitor and ginsenoside CK are combined to achieve a better killing effect on other various cancer cells, and it is indicated that improvement of the effect is broad-spectrum.

The invention discloses poplar and phellinus igniarius polysaccharide SVP-1 as well as a preparation method and application thereof, and belongs to the field of biological medicines. The poplar phellinus igniarius polysaccharide SVP-1 provided by the invention has remarkable anti-tumor activity, and can effectively inhibit proliferation, invasion and migration of tumor cells so as to block malignant progression of tumors. The structure is clear, the preparation method is controllable, the stability and biological activity of polysaccharide components are ensured, and a reliable basis is provided for development of antitumor drugs. When the traditional Chinese medicine composition is used together with radiotherapy and chemotherapy medicines, a synergistic effect can be achieved, the sensitivity of tumors to treatment can be improved, the toxic and side effects of radiotherapy and chemotherapy can be relieved, and the effects of reducing toxicity and increasing efficiency are achieved. According to the combined treatment strategy, the curative effect of the existing tumor therapy can be remarkably improved, meanwhile, adverse reactions are reduced, and a new optimization scheme is provided for clinical tumor treatment.

The present invention provides anticancer agents comprising as an active ingredient a bispecific antibody that comprises a domain comprising a glypican 3-binding antibody variable region, a domain comprising a T cell receptor complex-binding antibody variable region, and common L chains that can enhance the affinity for the two antigens, as well as pharmaceutical compositions comprising the bispecific antibody as an active ingredient, the compositions being for use in combination with other anticancer agents. The bispecific antibodies are novel molecules which are produced with high efficiency and have strong anti-tumor activity as well as safety and excellent pharmacodynamics. The bispecific antibodies can be expected to be applied to various cancers.

The present invention relates to a hetero (aromatic) ring-substituted cyclic diamine compound, the preparation thereof and the use thereof in the preparation of a drug for treating and / or preventing tumors. The structural formula of the compound is as shown in (I). The compound has a significant inhibitory effect on the growth of cells of tumors such as leukemia, lymphoma, breast cancer, melanoma, ovarian cancer, colorectal cancer, cervical cancer, lung cancer, prostate cancer, esophageal cancer, glioma, kidney cancer, nasopharyngeal carcinoma, liver cancer, gastric cancer and pancreatic cancer. Compared with the prior art, the compound of the present invention has a broad-spectrum anti-tumor activity, has a good effect on inhibiting tumors, and has an effect of degrading PD-L1 proteins, and is thus a PD-L1 immunomodulator.

The invention belongs to the field of biological medicine, and relates to an anti-EGFR monoclonal antibody, a bispecific antibody thereof, a pharmaceutical composition and application. Specifically, the invention relates to an anti-EGFR antibody or an antigen binding fragment thereof. The invention also relates to an anti-EGFR (Epidermal Growth Factor Receptor) and anti-MET (Methyl The anti-EGFR monoclonal antibody and the bispecific antibody provided by the invention both have good anti-tumor activity.

Provided are delivery immunostimulatory bacteria that have enhanced colonization of tumors, the tumor microenvironment and / or tumor-resident immune cells, and enhanced anti-tumor activity. The immunostimulatory bacteria are modified by deletion of genes encoding the flagella, or by modification of the genes so that functional flagella are not produced, and / or are modified by deletion of pagP or modification of pagP to produce inactive PagP product. As a result, the immunostimulatory bacteria are flagellin− and / or pagP−. The immunostimulatory bacteria optionally have additional genomic modifications so that the bacteria are adenosine or purine auxotrophs. The bacteria optionally are one or more of asd−, purI−, and msbB−. The immunostimulatory bacteria, such as Salmonella species, are modified to encode immunostimulatory proteins that confer anti-tumor activity in the tumor microenvironment, and / or are modified so that the bacteria preferentially infect immune cells in the tumor microenvironment, or tumor-resident immune cells, and / or are modified to induce less cell death in immune cells than in other cells. Also provided are methods of inhibiting the growth or reducing the volume of a solid tumor by administering the immunostimulatory bacteria.

The invention provides a pyrrolidone dihydroisoxazole compound as well as a preparation method and application thereof, and belongs to the technical field of organic synthesis. Specifically, under the catalytic action of Lewis base, beta-oxoacrylamide and 4-nitroisoxazole serve as raw materials, and the pyrrolidone dihydroisoxazole compound is synthesized through a one-step method. Beta-oxoacrylamide and 4-nitroisoxazole which are simple and easy to obtain are adopted as starting raw materials, dearomatization [3 + 2]-cycloaddition reaction is carried out under the catalysis of Lewis base, the pyrrolidone dihydroisoxazole compound is synthesized, the method is easy and convenient to operate and mild in reaction condition, the used reagents and raw materials are economical and easy to obtain, and the method is suitable for industrial production. The target product yield is high, the substrate application range is wide, and the in-vitro anti-tumor activity is good.

The invention provides a preparation method and application of a turmeric extracellular vesicle targeted drug delivery system with an anti-colon cancer effect. The engineering system of modifying CELNs and loading DOX by the TCP-1 colon cancer targeting peptide is constructed by extracting curcuma longa extracellular vesicles (CELNs). The system of loading adriamycin through targeted modified turmeric extracellular vesicles has better anti-tumor activity and tumor targeting property, and HE staining and serum detection results show that the system has no significant influence on important tissues, visceral organs and liver functions of mice. And the biological safety is improved while a better treatment effect is achieved.

The invention belongs to the field of chemical medicines, and particularly relates to a combined medicine for preventing and / or treating prostatic cancer, application of the combined medicine and a medicine composition. The combined medicine disclosed by the invention comprises immune cells with enhanced infiltration degree and a galectin-1 inhibitor; the immune cells with enhanced infiltration degree are natural killer (NK) cells with TTTY15-USP9Y chimera RNA knocked out, the infiltration degree and anti-tumor activity of the NK cells in a prostate cancer microenvironment can be improved, and the activated NK cells have a stronger killing effect on tumor cells in vitro. The immune cells with enhanced infiltration degree and the galectin-1 inhibitor are combined for use, so that the composition shows a synergistic effect in treatment of prostatic cancer, and has a wide application prospect.

The invention provides lucid ganoderma oligopeptide with an anti-tumor effect and a preparation method thereof. The three oligopeptides are separated and purified from the ganoderma lucidum for the first time, and the oligopeptides have broad-spectrum anti-tumor activity, can effectively inhibit tumor cell proliferation, have good biological compatibility and have great application prospects.