36results about How to "Significant inhibition of proliferation" patented technology

The invention discloses a nitrogen-containing fused heterocycle compound shown by a formula I, a pharmaceutically acceptable salt thereof, or enantiomers, diastereoisomers, tautomers, solvates, metabolic precursors or prodrugs of the nitrogen-containing fused heterocycle compound and the pharmaceutically acceptable salt thereof, or a pharmaceutical composition containing the nitrogen-containing fused heterocycle compound and an application of the nitrogen-containing fused heterocycle compound. The nitrogen-containing fused heterocycle compound disclosed by the invention has relatively good antitumor activity.

The invention discloses a quinazoline derivative and a pharmaceutically acceptable salt thereof showed in a formula I, or their enantiomer, diastereoisomer, tautomer, racemate, solvate, metabolic precursor or prodrug. The invention also discloses a preparation method, an intermediate, a composition and an application. The quinazoline derivative has good antineoplastic activity.

The invention discloses an oxadiazole-contained cyclic compound, a preparation method, intermediates, compositions and application thereof. The medically acceptable salts, the enantiomer, the diastereoisomer, the tautomer, the solvate, the metabolite or the prodrug of the dthe oxadiazole-contained cyclic compound shown as the formula I is high in inhibitory activity on IDO (dioxygenase) at a molecular level and a cellular level and significant in proliferation inhibition effects on cancer cells related to IDO activity at an animal level and good in liver microsome stability of human, mouse andthe like, has no significant inhibition over metabolic enzymes and achieves good absorption properties and high bioavailability in rats and mice as well as good druggability.

The invention relates to the field of genetic engineering, in particular to a novel fungal immunomodulatory protein FIP-NHA with antineoplastic activity and a gene thereof. The fungal immunomodulatory protein FIP-NHA according to the invention has an amino acid sequence as shown in SEQ ID NO. 1, and the gene fip-nha for coding the fungal immunomodulatory protein has a nucleotide sequence as shownin SEQ ID NO. 2. The fungal immunomodulatory protein FIP-NHA provided by the invention has the effects on promoting splenic lymphocyte division, increasing synthesis of interleukin 2, and obviously inhibiting proliferation of three tumor cells including hepatoma cell HepG2, gastric cancer cell MGC823 and leukemia cell HL60, therefore, the fungal immunomodulatory protein FIP-NHA as a novel antineoplastic biological agent can be widely used in the fields of health products and biological medicines.

The invention discloses a method for preparing an edible fungus protein extract with antitumor efficacy. The preparation method comprises the following steps of: 1) extracting by water after crushing edible fungus sporocarp, collecting a water-soluble matter to obtain an edible fungus water-soluble extract; 2) carrying out ammonium sulfate precipitation of which the saturation level is 80% on the edible fungus water-soluble extract, collecting sediments, and obtaining the edible fungus protein extract with the antitumor efficacy after dialyzing the sediments by deionized water, wherein the edible fungus is at least one of the following funguses: auricularia polytricha, pleurotus citrinopileatus, abalone mushroom, pycnoporus cin, cordyceps militaris, pleurotus djamor, black fungus, clitocybe maxima, flammulina velutipes, oudemansiella radicata and pholiota adipose. The edible fungus protein extract disclosed by the invention has a significant proliferation inhibition role on an HepG2 cell, an MCF-7 cell and an A-549 cell, and can be used for preparing a product for resisting tumors or tumor cells.

The invention discloses a nitrogen-containing fused heterocyclic compound, and a preparation method, an intermediate, a composition and an application thereof. The compound has a high inhibitory activity against different subtypes of CDK at the molecular level, has a good inhibitory activity against breast cancer cells at the cellular level, has a significant proliferation inhibition effect on tumor cells associated with the cyclin-dependent kinase activity at the animal level, and has the advantages of good stability of liver microsomes in humans and mice, no significant inhibition effect onmetabolic enzymes, good absorption properties in rats and mice, high bioavailability, and good drug-forming property.

The invention discloses a cordyceps militaris protein extract and an antitumor application thereof. The cordyceps militaris protein extract is prepared by a method comprising the following steps of: (1) crushing cordyceps militaris cystocarps, soaking with water, and collecting a water-soluble substance to obtain a cordyceps militaris water-soluble extract; and (2) performing ammonia sulfate precipitation of which the saturation degree is 80% on the cordyceps militaris water-soluble extract, collecting a deposit, and dialyzing the deposit by using deionized water to obtain the cordyceps militaris protein extract. The IC50 values, after the cordyceps militaris protein extract is used for treating human hepatic carcinoma HepG2 cells, human mammary cancer MCF-7 cells and human lung adenocarcinoma A-549 cells for 72 hours, respectively are 10 microgram/mL, 14 microgram/mL and 8 microgram/mL, and the inhibition rates are increased along with the expansion of time and increase of concentration; and the changes of apoptotic forms can be observed under a light microscope.

The invention relates to poly-substitution flavane thiadiazoles class compound that uses neighbor hydroxy benzenes diketone and aromaticacid as raw material, taking concentrating and cyclization to gain flavanone class compounding that would react with substituted benzene to gain flavanone-4-phenylhydrazone, phenylhydrazone would cyclizating with thionyl chloride to form poly-substitution flavane thiadiazoles class compound. The invention has restraining function to kinds of tumor cell, and could be used in manufacturing anticancer medicine.

The invention discloses a 2-(3,4-dimethoxy)benzoyl-5-(4-substituted phenylethynyl) thiophene. The structural formula of the 2-(3,4-dimethoxy)benzoyl-5-(4-Substituted phenylethynyl) thiophene is as shown in the specification. The preparation method of the 2-(3,4-dimethoxy)benzoyl-5-(4-Substituted phenylethynyl) thiophene comprises the following steps: 1) reacting 2-bromothiophene with 3,4-dimethoxybenzoyl in a solvent in the presence of a catalyst and then carrying out purification and separation to obtain 2-(3,4-dimethoxy)benzoyl-5-bromothiophene; 2) reacting the 2-(3,4-dimethoxy)benzoyl-5-bromothiophene with 4-substituted phenylacetylene in a solvent in the presence of tetra(triphenylphosphine) palladium, CuI and an acid-binding agent, and then carrying out subsequent purification and separation. The invention also relates to application of the compound in preparation of anti-breast cancer targeted treatment drugs, and an application of the compound in preparation of anti-breast cancer resistance-reversal agents. The compound has relatively obvious proliferation inhibition effect on human breast cancer cells and breast cancer cell drug-resistant strains, and thus can be applied to preparation of the anti-breast cancer targeted treatment drug and the anti-breast cancer resistance-reversal agent. The compound has the potential of large-scale industrial production and relatively low cost.

The invention relates to application of a compound shown in a formula I in preparation of a medicine for preventing, delaying or treating NEDDylation modification pathway participated or mediated diseases, in particular to application in the anti-tumor field. A biological activity test result shows that the compound shown in the formula I has an effect of blocking an NEDDylation modification pathway and also has a remarkable proliferation inhibition effect. Therefore, the compound shown in the formula I can be used for developing antitumor drugs.

The invention discloses a nitrogen-containing heterocyclic compound as well as a preparation method and application thereof. The compound is shown as a formula I. The compound has relatively high inhibitory activity on different CDK subtypes at a molecular level; the inhibitory activity on breast cancer cells at the cellular level is relatively good; the compound has a remarkable proliferation inhibition effect on tumor cells related to cyclin-dependent kinase activity at an animal level, has good stability on liver microsomes of human beings, mice and the like, does not obviously inhibit metabolic enzymes, has good in-vivo absorbability and high bioavailability in rats and mice, and has relatively good druggability.