37results about How to "Antitumor activity" patented technology

An objective of the present invention is to provide novel compounds which have inhibitory activity against autophosphorylation of an FGF receptor family and, when orally or intraveneously administered, can suppress the growth of cancer cells. The compounds of the present invention are represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof:wherein X represents CH or N; Z represents O or S; Q represents NR10, CR11R2, carbonyl, O, S(═O)m, wherein m is 0 to 2, or urea; R1 to R3 each independently represent H, OH, halogen, nitro, amino, alkyl, alkoxy or the like in which the alkyl and alkoxy groups are optionally substituted; R4 represents H; R5 to R8 each independently represent H, halogen, alkyl, or alkoxy; and R9 represents an optionally substituted carbocyclic or heterocyclic group.

Disclosed herein are peptides which include an isoDGR motif and which selectively inhibit αvβ3 integrin. In some embodiments, the isoDGR motif results from the deamidation of an NGR motif.

Cytokine derivatives capable of homing the tumoral vessels and the antigen presenting cells and the use thereof as antitumoral agents.

A drug product which can maximize the effect of a cholestanol glycoside useful as an anticancer agent. The present invention provides a liposomal composition containing a glycoside exhibiting antitumor activity, a phospholipid, and a positive-charge-providing substance; the glycoside being composed of GlcNAc-Gal-, GlcNAc-Gal-Glc-, Fuc-Gal-, Gal-Glc-, or Gal- as a sugar moiety, and a hydrophobic compound capable of forming a liposome.

The invention discloses panax japonicus polysaccharide. The main chain structure thereof is Beta-1 to 4-D glucan and heterosaccharide containing mannan, galactan and xylan branched chain, the weight-average molecular weight of the panax japonicus polysaccharide is 5,000 to 200,000, the intrinsic viscosity at 25 DEG C is 1 to 50ml / g, and the mole ratio of the three elements of C: H: O is 1: 2: 1. The method for preparing the panax japonicus polysaccharide comprises the following steps: after being dried, smashed and skimmed, the panax japonicus is extracted by neutral salt water solution or pure water, and the white panax japonicus polysaccharide which can be easily dissolved in water, be dissolved in DMSO and not be dissolved in methanol, ethanol and acetone is obtained by separation, saponin removal, decolorization, dehydration, protein removal, desalination and drying. The panax japonicus polysaccharide which is prepared by the invention has higher anti-tumor activity and promotion of immune activity, which can be used for preparing drugs or health care products for improving immune function and anti-tumor. The method for preparing the product is simple and easy to operation, and the sources of the needed raw materials are wide.

The invention discloses panax japonicus polysaccharide.The main chain structure thereof is Beta-D-1 to 3-mannan and / or Alpha-D-3 to 4-mannan and heterosaccharide containing galactan, xylan and glucan, the weight-average molecular weight of the panax japonicus polysaccharide is 5,000 to 2,000,000, the intrinsic viscosity at 25 DEG C is 1 to 100ml / g, and the mole ratio of the three elements of C: H: O is 1: 2: 1. The preparation of the panax japonicus polysaccharide comprises the following steps: after being dried, smashed and skimmed, the panax japonicus is soaked by water under the normal temperature and is stirred for separation, the residue is extracted by high-pressure hot water, further extracted by alkali and reductive salt, and finally extracted by acid, and the panax japonicus polysaccharide which can be dissolved in water and DMSO and not be dissolved in methanol, ethanol and acetone is obtained by separation, neutralization by taking the solution, dehydration, protein removal, decolorization, desalination and drying. The panax japonicus polysaccharide which is prepared by the invention has higher anti-tumor activity and promotion of immune activity, which can be used for preparing drugs or health care products for improving immune function and anti-tumor. The method for preparing the product is simple and easy to operation, and the sources of the needed raw materials are wide.

The invention relates to the technical field of nano-selenium hydrosol, in particular to a nano-selenium hydrosol with anti-tumor activity and its preparation, preservation method and application. The hydrosol at least contains components with the following concentrations: 0.5mmol / L-5.0mmol / L of nano-selenium; 100.0mg / L-600.0mg / L of versicolor polysaccharide protein. The preparation method of the hydrosol at least includes step S01. adding a solution containing selenium ions and / or selenium ions to the polysaccharide protein aqueous solution of versicolor versicolor; step S02. adding a reducing agent solution dropwise to the mixed solution obtained in step S01, and shaking; Step S03. The product obtained from the reduction reaction in step S02 is subjected to constant volume and dialysis treatment. The hydrosol exists stably at 2-10°C. Because the polysaccharide protein of Yunzhi polysaccharide has hydrophilic hydroxyl and amino groups, these two groups can enhance the affinity between nano-selenium and cancer cells, increase the uptake of nano-selenium by tumor cells, and then reduce the dosage of drugs and increase the curative effect The overall therapeutic effect with less toxic and side effects provides a more effective solution for clinical combination chemotherapy of cancer.

A DDS preparation of a platinum complex, which selectively releases a highly active platinum complex in cells that are under reducing conditions, and exhibits high antitumor activity that is required from a medicine, is still not available, and there is a demand for a novel DDS preparation of a platinum complex that may be used in clinical fields. There is provided a polymer conjugate of a hexa-coordinated platinum complex, the polymer conjugate comprising a block copolymer having a polyethylene glycol structural moiety and a polyaspartic acid moiety or a polyglutamic acid moiety; and a hexa-coordinated platinum complex having a halogen atom and a hydroxyl group at the axial positions, the hexa-coordinated platinum complex being bonded, directly or via a spacer, to a side-chain carboxyl group of the block copolymer.

The novel C10-modified camptothecin analogs, and pharmaceutically-acceptable salts thereof, of the present invention: (i) possess potent antitumor activity (i.e., in nanomolar or subnanomolar concentrations) for inhibiting the growth of human and animal tumor cells in vitro; (ii) are potent inhibition of Topoisomerase I; (iii) lack of susceptibility to MDR / MRP drug resistance; (iv) require no metabolic drug activation: (v) lack glucuronidation of the A-ring or B-ring; (vi) reduce drug-binding affinity to plasma proteins; (vii) maintain lactone stability; (viii) maintain drug potency; and (ix) possess a low molecular weight (e.g., MW<600).

A DDS preparation of a platinum complex, which exhibits a superior antitumor effect required as a medicine and reduced side effects, that is, a clinically usable DDS preparation of a platinum complex, which is conjugated to a polymer carrier that is different from conventional carriers, is desired.Provided is a polymer conjugate of a platinum(II) complex, the polymer conjugate including: a block copolymer having a polyethylene glycol structural moiety and a polyaspartic acid moiety or a polyglutamic acid moiety; a sulfoxide derivative introduced into a side-chain carboxyl group of the block copolymer; and a platinum(II) complex coordinate-bonded to a sulfoxide group of the sulfoxide derivative.

The invention relates to the field of medicinal chemistry and in particular relates to an imidazole [4,5-c] pyridine-7-methanamide derivative (I), wherein R is defined in the specification. Pharmacodynamic tests proof that the derivative compound provided by the invention can serve as a tumour therapeutic agent and especially the derivative compound has extremely strong anti-tumour effect when being combined with cis-platinum. The invention also discloses a preparation method of the derivative compound and a pharmaceutical composition comprising the derivative compound.

The invention provides a blood group A epitope mimic peptide. The amino acid sequence of the peptide is Tyr-Val-Asp-Ser-Lys-Ala-Phe-Arg-Ala-Val-Val-Arg. The blood group A epitope mimic peptide can mimic carbohydrate epitope of blood group A and is used for preparing anti-tumor DNA vaccines. The invention also provides the anti-tumor DNA vaccines which are constructed by inserting the genes codingthe peptide according to the claim 1 and the fusion protein with intracellular domain of Fas into the multiple clone sites of the pIRES plasmids. After being injected into part of the tumor, the DNA vaccines can be absorbed by the tumor cells and express the mimic peptide and the fusion protein of the anti-tumor factors so that the mimic peptide is bonded with the complement and the naturally existing antibody to give play to CDC and ADCC to kill the tumor cells.