38 results about "Antineoplastic Drugs" patented technology

The present invention discloses an antitumor pharmaceutical composition based on immune checkpoint blockade and its application, which comprises paroxetine hydrochloride and a T cell enhancer, which is at least one of vitamin E and thymosin. Through a series of in vitro and in vivo experiments, the present invention has first discovered that cannabidiol and paroxetine hydrochloride can effectively reduce the expression of PD-L1 on the surface of tumor cells, block the PD-1 / PD-L1 signaling pathway, and enhance the tumor cell killing effect of T cells. Based on this, the addition of a T cell enhancer can further increase the number and activity of T cells, significantly enhancing the killing ability of T cells after immunosuppression is released, thereby significantly enhancing the antitumor effect of the drug. The components of the pharmaceutical composition of the present invention, cannabidiol, paroxetine hydrochloride, vitamin E, and thymosin, exert a synergistic effect, improving the antitumor effect.

The application belongs to the technical field of antitumor drugs, and particularly relates to an AuNRs@L / D-Ag2S QDs complex, a preparation method and application thereof. Sodium polystyrene sulfonate is electrostatically adsorbed on AuNRs to obtain 1-PSS-AuNRs; polyallylamine hydrochloride is electrostatically adsorbed on 1-PSS-AuNRs to obtain 2-PAH-AuNRs; polyallylamine hydrochloride is electrostatically adsorbed on 2-PAH-AuNRs to obtain a non-chiral nanomaterial; and the non-chiral nanomaterial is covalently crosslinked with L / D-Ag2S QDs to obtain the AuNRs@L / D-Ag2S QDs complex. The application combines the efficient photo-thermal conversion characteristics of AuNRs with the chiral-dependent targeting and potential fluorescence imaging ability of chiral Ag2S quantum dots by constructing a complex structure, so that a novel nanodiagnostic and therapeutic agent with efficient photo-thermal performance and chiral selectivity is obtained.

The application discloses a high-activity 8-hydroxyquinoline rhodium complex in vivo and in vitro and a synthesis method and application thereof. The 5,7-dichloro-8-hydroxy-2-methylquinoline, dichloro (pentamethylcyclopentadienyl) rhodium (III) dimer, methanol, dimethyl sulfoxide and triethylamine are taken, and under a closed condition, the reaction is carried out at 80 DEG C for 3 days; after being cooled to 37 DEG C, filtration and drying are carried out, and the 5-chloro-8-hydroxyquinoline rhodium complex is obtained. The 5-chloro-8-hydroxyquinoline rhodium complex has obvious inhibiting effect on SK-OV-3 and SK-OV-3 / DDP cancer cells, shows superior antitumor activity, and has small toxicity to normal HL-7702 cells; the 5-chloro-8-hydroxyquinoline rhodium complex has potential medicinal value and is expected to be used for preparation of various antitumor drugs.

This invention provides an antitumor drug with excellent therapeutic effects, exhibiting superior antitumor efficacy and safety. It also provides an anti-cadherin 17 antibody comprising a heavy chain variable region and a light chain variable region, a drug conjugate thereof, and a composition containing an anti-cadherin 17 antibody or a drug conjugate thereof, and their use as a drug.

This invention belongs to the field of biomedical technology and discloses an alginate-based thermosensitive amphiphilic drug-loaded nanoparticle composite gel. It comprises a combination of thermosensitive amphiphilic modified alginate material, amphiphilic modified alginate, thermosensitive modified alginate material, and alginate material. This gel forms ionic crosslinks initiated by an ionic crosslinking agent, and simultaneously, at a human body temperature of 37-38°C, chemical crosslinks are initiated to form a more stable gel. Furthermore, this gel simultaneously achieves the sustained and slow release of the encapsulated antitumor drug.

The application belongs to the field of antitumor drug chemistry, and discloses application of a selective PRMT4 inhibitor, deacetylganoderic acid F, in a drug for resisting drug-resistant osteosarcoma. The deacetylganoderic acid F has the following structure: it forms a unique hydrogen bond effect and binding mode with PRMT4, is a PRMT4 selective inhibitor, has the characteristics of strong enzyme inhibition selectivity, small toxic and side effects, and strong anti-drug-resistant osteosarcoma effect, and can be used as an anti-drug-resistant osteosarcoma drug. Mechanism research shows that the deacetylganoderic acid F can regulate the active oxygen level to play an anti-drug-resistant osteosarcoma role. The problems of poor selectivity and large toxic and side effects of existing PRMT4 inhibitors are solved, and a new drug selection is provided for the treatment of drug-resistant osteosarcoma.

The application provides imidazotetrazine compounds or pharmaceutically acceptable salts thereof, and a preparation method and application thereof, and belongs to the technical field of medicines. The imidazotetrazine compounds or pharmaceutically acceptable salts thereof are obtained by connecting valproic acid, chlorambucil and borneol to an imidazotetrazine group through an ester bond or an amide bond by using a splicing principle. The imidazotetrazine compounds or pharmaceutically acceptable salts thereof have better antitumor activity, and a new generation of powerful antitumor drugs can be developed.

The application provides an antitumor drug, a preparation method and application thereof, and belongs to the technical field of medicines. 4 The Fe3O NPs are deposited with polydopamine on the surface, then a COF layer is formed on the surface through a one-pot method, and an antitumor compound is loaded; further, doxorubicin is loaded on the surface, and then the antitumor drug is prepared by reacting with F127 coupled with folate and oligomeric hyaluronic acid. The antitumor drug prepared by the application has high anticancer activity and drug resistance reversal, high drug loading rate, is not prone to aggregation, has good biocompatibility, good targeting and slow release, and has good application in chemotherapy, photodynamic therapy, photothermal therapy and nuclear magnetic imaging, so that the antitumor drug becomes a new generation of diagnosis and treatment integrated reagent.

Disclosed are pyrrolopyrimidine derivatives as Wee-1 inhibitors. Specifically, the application relates to a compound shown in a general formula (1) and a preparation method thereof, and the use of the compound shown in the general formula (1) and each isomer, each crystal form, a pharmaceutically acceptable salt, a hydrate or a solvate of the compound as Wee-1 inhibitors in the preparation of antitumor drugs.

The application belongs to the field of antitumor drug preparation, and particularly relates to albumin binding and non-binding gemcitabine prodrugs, and a preparation method and application thereof. The acryloyl chloride gemcitabine prodrug is a compound formed by bridging gemcitabine and acryloyl chloride through an amide bond, and the two non-albumin binding prodrugs are compounds formed by bridging gemcitabine and 3-succinimidyl propionic acid / propionic acid through an amide bond. The ethylene group in the prodrug is a binding target for the free thiol group of the 34th cysteine on albumin, can be rapidly and specifically combined with albumin in the systemic circulation, and further forms an albumin prodrug complex. The complex can significantly improve the stability of gemcitabine in the systemic circulation, and prolong the systemic circulation time. The macromolecular prodrug strategy designed in the application can improve the delivery efficiency of chemotherapeutic drugs, improve the antitumor effect of chemotherapeutic drugs, and provides a new direction and new ideas for the delivery of chemotherapeutic drugs.

This invention discloses an endophytic fungus of *Aspergillus sp.* and its applications. The invention provides a novel endophytic fungus, PS4, which possesses unique antibacterial and antitumor activities. The secondary metabolites produced during fermentation contain various active ingredients, such as shikonin, 10-hydroxycamptothecin, and rhodioloside, exhibiting significant antioxidant, antibacterial, and antitumor effects. Simultaneously, the controllable fermentation process of the endophytic fungus improves the stability and yield of the product. The use of bio-fermentation is more environmentally friendly, reducing environmental impact, and ultimately provides a new option for clinical treatment, especially in combating drug-resistant strains and antitumor drugs.

This invention discloses a benzamide / benzenesulfonamide compound containing an aryl butanone structure, its preparation method, and its application, belonging to the field of medicinal chemistry. The structure of the benzamide compound containing the aryl butanone structure is as follows: R1 is hydrogen, halogen, alkyl, or alkoxy; R2 is tert-butyl, tert-pentyl, tert-octyl, adamantyl, or α,α-dimethylbenzyl; R3 is hydrogen, halogen, alkyl, alkoxy, fused ring, or aryl; R4 is hydrogen, alkyl, or aryl. The structure of the benzenesulfonamide compound containing the aryl butanone structure is as follows: R1 is hydrogen, halogen, or alkyl; R2 is tert-butyl, tert-pentyl, or tert-octyl; R3 is hydrogen, halogen, alkyl, or fused ring. The advantages of this invention are that some of the prepared compounds exhibit strong inhibitory effects on MCF-7 and HCT-116, and can be used as lead compounds for the subsequent preparation and development of antitumor drugs.

The application discloses a drug sustained-release elastic embolism microsphere and a preparation method and application thereof, and belongs to the technical field of medical materials. The application is prepared by the following steps: taking an acetic acid aqueous solution in which chitosan is dissolved as a dispersed phase, mixing the dispersed phase and a continuous phase into a W / O monodisperse emulsion template through microfluidic technology, introducing the W / O monodisperse emulsion template into an acceptant phase containing genipin, a W / O surfactant and an organic oil, crosslinking under magnetic stirring for 4-24 hours, post-treating the obtained microspheres to obtain elastic embolism microspheres, and finally dispersing the elastic embolism microspheres in an impregnation liquid in which a hydrophilic antitumor drug is dissolved and performing oscillation treatment, so that the drug sustained-release elastic embolism microsphere is prepared. The application effectively optimizes the drug loading capacity and drug sustained-release performance of the formed microspheres by setting the single chitosan dispersed phase component and adopting the technical strategy of jointly regulating and controlling the microfluidic control emulsification and crosslinking time, so that the effect of simply preparing the drug sustained-release elastic embolism microsphere is achieved.

The application discloses use of self-assembled polymers for antibacterial, antitumor drug delivery, preparation of synergistic antibacterial drugs or antitumor drugs.

The application provides a 1-heteroaryl-3-sulfone group bicyclo[1.1.1]pentane compound and a preparation method and application thereof, and belongs to the technical field of synthesis of pharmaceutical intermediates. The compound provided by the application is a double-substituted bicyclo[1.1.1]pentane containing a sulfone group and a heteroaryl group and derivatives thereof, wherein the sulfone group is an important pharmacophore, plays a role in antitumor drugs by participating in hydrogen bond interaction, regulating cell signaling pathways and the like, and the series of compounds have antitumor activity. The application uses cheap and easily available sulfonic acid chlorides, [1.1.1]spiro propeller and heteroaromatic compounds as raw materials, and prepares a series of sulfone group and heteroaryl group double-substituted bicyclo[1.1.1]pentane under mild conditions through a three-component tandem reaction with high selectivity and high yield, and the preparation method is simple and suitable for industrial production.

This invention discloses the application of the combined use of tanshinone and decitabine in the preparation of drugs for treating breast cancer, belonging to the field of antitumor drug application technology. This invention reveals a novel mechanism by which the combined use of tanshinone (Miltirone) and decitabine (DAC) inhibits breast cancer development by inducing pyroptosis and inhibiting epithelial-mesenchymal transition (EMT). Experimental verification shows that the combined treatment of Miltirone and DAC significantly reduces the viability of 4T1 breast cancer cells, inhibiting their proliferation, migration, and invasion abilities; simultaneously, this combined regimen induces significant pyroptosis by promoting the cleavage of pyroptosis-related proteins such as GSDME, accompanied by an increase in the release of LDH and ATP. This invention provides important experimental evidence and new ideas for the development of combination therapy strategies for breast cancer and the preparation of highly effective pyroptosis-inducing antitumor drugs.

The application provides an antitumor pharmaceutical composition and application thereof, and belongs to the field of pharmacy. The antitumor pharmaceutical composition is composed of 5-fluorouracil and paclitaxel; the weight ratio of the 5-fluorouracil and the paclitaxel is 2:(2.3-10). Researches show that the 5-FU and the PTX with the specific weight ratio have a synergistic effect on inhibiting the proliferation of breast cancer cells in a certain concentration range. The 5-FU and the PTX with the specific weight ratio can be used for preparing a drug for treating breast cancer, and have a good application prospect.

The application discloses a novel alkaloid compound extracted from Portulaca oleracea and an extraction method thereof, and belongs to the field of traditional Chinese medicine extraction and separation. 19 H 32 N2O9, and is named as 2-((5-((2-amino-4,5-dimethylphenyl)amino)-2,3,4-trihydroxypentyl)oxy)-6-(hydroxymethyl)tetrahydro-2H-pyran-3,4,5-triol according to the structure. The application further discloses an extraction and separation method of the compound, which comprises the following steps: after Portulaca oleracea medicinal materials are extracted by refluxing with 50% ethanol, the residue is extracted with water, and then subjected to macroporous resin adsorption, ODS column chromatography, Sephadex LH-20 dextran gel column chromatography and UHPLC separation and purification to obtain the target compound. The compound has anti-inflammatory and antitumor activities, and can be used for preparing anti-inflammatory or antitumor drugs.

This invention discloses an anti-drug-resistant lung cancer compound, its preparation method, and its applications. The invention involves reacting 5-chloro-8-hydroxyquinoline, dichloro(pentamethylcyclopentadienyl)rhodium(III) dimer, methanol, dimethyl sulfoxide, and triethylamine under sealed conditions at 80 °C for 3 days. After cooling to 37 °C, the mixture is filtered and dried to obtain the final product. The 5-chloro-8-hydroxyquinoline rhodium complex exhibits superior antitumor activity by targeting and inhibiting the growth of lung cancer cells A549 and cisplatin-resistant lung cancer cells A549 / DDP, while showing low toxicity to normal HL-7702 cells. It possesses potential pharmaceutical value and is expected to be used in the preparation of various antitumor drugs.

The present application relates to the technical field of anticancer chemicals, in particular to a thiazole four-core copper complex with antitumor and antibacterial activity, and a preparation method and application thereof.The chemical formula of the complex is [Cu4(C3H3S2N2)2(C3H4S2N2)4], which is synthesized from a ligand thiazole and CuX, wherein X is I or Br, and the copper in the obtained complex is +1 valence.The complex shows good cytotoxicity on breast cancer cells MCF-7, and is likely to exert toxic effects through multiple pathways such as induction of cell apoptosis, ferroptosis and cupric death, and has good antibacterial effect, has potential medicinal value, and is expected to be developed into a new generation of antitumor drugs with antibacterial performance.

This invention belongs to the field of pharmaceutical technology, specifically relating to a class of sarpagine-type indole alkaloid derivatives, their preparation methods, and applications. The structural formula of this class of compounds is shown in formula (I). They exhibit good antitumor activity, low toxicity to normal cells, and are safe, effective, and low-toxicity candidate antitumor drugs.

This invention relates to the field of novel compounds from the field of bald cypress, and provides an antitumor active compound, its preparation method, and its application. The antitumor active compound provided by this invention ( Taiwanin J This compound, a secondary metabolite of *Cephalotaxus fortunei*, belongs to the lignan class of compounds. Its antitumor activity enriches the diversity of lignan compounds and exhibits significant inhibitory activity against HeLa and A549 cells, showing broad application prospects in the preparation of antitumor drugs. Furthermore, it can serve as a lead compound, which is of great significance for the development of novel antitumor drugs. This invention also provides a method for preparing the antitumor active compound described above. The preparation method provided by this invention is simple to operate, low in cost, and easy to implement industrially. Moreover, this invention uses *Cephalotaxus fortunei* stem bark as raw material for extraction, achieving effective utilization of this rare plant resource, which aligns with the concepts of green environmental protection and a low-carbon economy.

The present invention relates to combinations comprising N-{3-[4-Amino-7-(1-methyl-piperidin-4-yl)-7H-pyrrolo[2,3- d]pyrimidin-5-yl]-2-fluoro-phenyl}-5-chloro-2-fluoro-4-methoxy-benzenesulfonamide or its pharmaceutically acceptable salt and antineoplastic agents. The invention also relates to the use of said combination in the treatment of cancer.

The present invention pertains to a peptide of the S100A1 protein for use in the treatment or prevention of antineoplastic agent-mediated cytotoxicity or cancer therapy-related cardiac dysfunction (CTRCD) or cancer therapy-related heart failure (CTRHF), as well as nucleic acids encoding said peptide, vectors comprising said nucleic acid, host cells comprising the vector or nucleic acid and expressing it, and to respective pharmaceutical compositions.

This invention discloses a method for preparing acid-responsive water-soluble fullerene nanoparticles. The method includes the following steps: S1, performing a Prato reaction on a fullerene material, a glycine derivative, and a carboxyl-containing compound to obtain a fullerene derivative with carboxyl-terminated ends; S2, performing an esterification reaction on the fullerene derivative with carboxyl-terminated ends and a water-soluble polymer in an organic solvent B under the action of a catalyst to obtain a water-soluble fullerene derivative; S3, performing a condensation reaction on an amino acid and a compound with aldehyde-terminated ends under alkaline conditions to obtain an amino acid derivative with acid-responsive properties; S4, mixing the water-soluble fullerene derivative and the amino acid derivative with acid-responsive properties in water to composite them, obtaining acid-responsive water-soluble fullerene nanoparticles. This method has advantages such as suitable size, stable properties, good biosafety, and simple preparation method, and can be applied to the preparation of antitumor drugs.

The application relates to the fields of biological medicine and high polymer materials, and discloses a sustained-release implant type biodegradable stent loaded with an antitumor active component, which is composed of polylactic acid-glycolic acid copolymer, doxorubicin hydrochloride, citric acid-terminated polyethylene glycol polymer, zinc acetate dihydrate and N-acetyl cysteine. The metastable complex structure is constructed by in-situ coordination reaction between the components, so that the rapid release of the water-soluble doxorubicin hydrochloride in the initial implantation stage is blocked. After implantation, N-acetyl cysteine is preferentially dissociated and released, so that the zinc ion coordination unsaturated sites are generated in the coordination network; with the hydrolysis of the polylactic acid-glycolic acid copolymer, the generated lactic acid molecules intervene in the above unsaturated sites to generate a competitive coordination reaction, so that the coordination skeleton is destroyed and the antitumor drug is released. The application realizes the synchronization of the drug release rate and the high polymer matrix degradation rate, and the acetate dissociated from the zinc acetate can effectively buffer the pH value of the degradation microenvironment.