33results about How to "Broad-spectrum antitumor activity" patented technology

The invention relates to a nicotinic acid derivative shown in the formula (I), and pharmaceutically acceptable salt or solvate thereof, wherein Z is selected from O, S and NR3, and R3 is hydrogen or C1-6 alkyl; R1 or R2 is independently selected from hydrogen, C1-6 alkyl, C1-6 alkoxy group, halogenated C1-6 alkyl, halogen, nitro, aryl, aryl oxygroup, heteroaryl, heteroaryl oxygroup, heterocyclic radical, and heterocyclic oxygroup; C1-6 alkoxy group, halogenated C1-6 alkyl, aryl, heteroaryl, and heterocyclic radical can be optionally substituted by substituent groups which can be C1-6 alkyl, C1-6 alkoxy group, halogenated C1-6 alkyl, halogen, cycano, nitro and aryl; m is an integer of 0 to 4; and n is an integer of 0 to 5. The compound or salts thereof have strong inhibition activity to colorectal cancer cell line HCT-116, human lung cancer cell line A549 and breast cancer cell line MCF-7. In addition, the compound is broad-spectrum in anti-cancer activity, and can be used as a candidate drug or a pilot compound for treating diseases of tumors, cancers and the like.

The invention provides a fructus sophorae total flavonoid extract with broad-spectrum anti-tumor activity and a preparation method and application of the fructus sophorae total flavonoid extract. The fructus sophorae total flavonoid extract at least comprises quercetin, genistein, kaempferol and isorhamnetin according to the mass ratio of (2-3): (14-16): (15-17): (0.5-1), and has a favorable in-vitro anti-oxidative function, broad-spectrum anti-tumor activity, and a remarkable inhibiting effect on human esophagus cancer, liver cancer, breast cancer, human lymphoma and the like. The preparation method comprises the following steps: taking nut parts of fructus sophorae in autumn as the raw materials; then taking ethanol of 80 percent, 60 percent and 40 percent volume fractions as solvents for gradient ultrasonic extraction, macroporous adsorption resin adsorption and elution; collecting the eluant; concentrating and drying. The preparation method remarkably improves the extraction ratio of fructus sophorae total flavonoids, simplifies the extraction steps and reduces impurity interference.

The invention relates to garcinia acid amide derivative and preparation method thereof and purpose, and the structural formula of the derivative is shown as formula (I); The preparation method comprises the following steps: garcinia acid and nucleoside medicament or salt nucleoside of nucleoside medicament melted in an inertia solvent under room temperature; then a catalyzed condensation reagent is added for reaction for 3 to 5 hours by blending at the temperature between 40 and 60 DEG C; and garcinia acid amide derivative is obtained after washing, drying, distillation andn column chromatography. The derivative of the present invention can be used for used to prepare compositions, antineoplastic drugs, antimycotics drugs or anti-angiogenic drugs generation medicament or be used with other anticancer active components. The compound of the present invention not only displays better activity to a plurality of tumor cells, shows good targeting to tumor cells, which makes a good foundation for novel medicament exploitation.

The invention belongs to the field of medicinal chemistry and relates to an isonicotinic acid derivative with a novel structure as well as a preparation method and use thereof. The invention mainly relates to the isonicotinic acid derivative, a stereisomer, a racemate, a tautomer or pharmaceutically acceptable salt which is represented by a formula (I) (shown the description), pharmaceutically acceptable salt thereof, a preparation method thereof and use thereof in the preparation of anti-cancer drugs. In the formula (I), Z is selected from O, S and NR3, R3 represents hydrogen or C1-C6 alkyl;R1 is selected from C1-C6 alkyl, C1-C6 alkoxy, halogenated C1-C6 alkyl, aryl, aryloxy, heteroaryl, heteroaryloxy, a heterocyclic radical, a heteroepoxy group or halogen; R2 is selected from halogen, cyan, C1-C6 alkyl, C1-C6 alkoxy or halogenated C1-C6 alkyl; m represents an integer of 0-4; n represents an integer of 0-5; and the condition is that R2 is not halogen when Z is selected from NR3, m is0 and n is 1.

The invention discloses a compound containing an indole structure, a preparation method and the application of the NEDD8 activating enzyme as a target in antitumor drugs, and belongs to the field of medicinal chemistry. The indole derivative of the present invention has the following structure: the anticancer activity test in vitro shows that the compound I-1 has a certain inhibitory effect on various tumor cells. Enzyme inhibition experiments prove that indole derivative I‑1 selectively inhibits the activity of NEDD8 activating enzyme, which is valuable for studying the biological function of NEDD8 activating enzyme and developing NEDD8 activating enzyme inhibitor antitumor drugs.

The invention discloses a quinoline derivative as shown in the formula (I) in the specification and a salt of the quinoline derivative, wherein in the formula, Z is NH or O; R is selected from hydrogen, fluorine, chlorine, bromine, methyl, ethyl, tertiary butyl, trifluoromethyl, methoxyl or nitryl; n is an integer of 0, 1, 2 or 3. The invention relates to a preparation method and application of the compound as shown in the formula (I) in the specification and the salt of the compound. The compound or the salt has very high inhibition activity for a human lung cancer cell strain A549, a colorectal cancer cell strain HCT-116 and a breast cancer cell strain MCF-7. The compound has a broad-spectrum anti-cancer activity and can be used as a candidate medicine or a lead compound for treating diseases such as tumor and cancer.

The invention relates to the technical field of medicines and particularly relates to pseudolarix acid derivatives with the structure shown in a formula (1) (the detailed definitions of all groups are shown in the specification). The compounds have favorable activity for various tumor cells such as human lung cancer, colon cancer, breast cancer and the like; besides, the compounds show better antifungal activity. The invention also discloses a composition and preparation method of the pseudolarix acid derivatives as well as the application of the seudolarix acid derivatives in preparation of antitumor medicaments, antifungal medicaments or anti-angiogenesis medicaments.

A seven-element-ring berberine analogue and pharmaceutically acceptable salt thereof. The seven-element-ring berberine analogue has the structure shown by formula A, and the definition of each substituted radical is as defined in the specification. Also provided are a preparation method of the seven-element-ring berberine analogue represented by formula A, and a use thereof in preparing medicine for preventing or treating tumors or cancer.

The invention relates to a gambogic acid ester derivative as well as a preparation method and a use thereof. The structural formula of the derivative is as shown in formula (I) in the specification. The preparation method of the gambogic acid ester derivative comprises the following steps of: dissolving gambogic acid, gemcitabine and triphenylphosphine in anhydrous tetrahydrofuran under the protection of nitrogen gas; injecting a THF (Tetrahydrofuran) solution containing Diethyl Azodicarboxylate (DEAD) and reacting for 12-24 hours; and obtaining a product by washing, drying, rotary steaming and column chromatography. The derivative can be used for preparing a composition, an antineoplastic drug, an antifungal drug or an anti-angiogenic drug or is combined with other anti-cancer active components. The derivative disclosed by the invention not only has good activity to a plurality of tumor cells, but also has good targeting performance to the tumor cells, and therefore, a foundation is laid for developing novel drugs.

The invention relates to a metronidazole derivative shown in the formula (1) (please see the specific formula in the specification) and salt or solvate which can be accept by the metronidazole derivative on the pharmaceutical science. R can be the same or different and can be independently selected from hydrogen, halogen, a cyano group, nitro, C1-C6 alkyl, C1-C6 alkoxy, halogenation C1-C6 alkyl, halogenation C1-C6 alkoxy, aryl, aryloxy and the like, and n is an integer from 0 to 4. The invention further relates to a preparing method and application of the metronidazole derivative in the formula (I). The compound or the salt of the compound has the strong inhibitory activity on the colorectal cancer cell strain HCT-116, the human lung cancer cell strain A549 and the breast cancer cell strain MCF-7. The compound has broad spectrum on anti-cancer activity and can serve as candidate medicine or a lead compound for treating tumors, cancers and other diseases.

The invention discloses a polydiselenium carbonate polymer and an application thereof. Repeat units of the polymer are as shown in the specification, wherein P is an integer from 20 to 450, m is an integer from 1 to 40, and n is an integer from 10 to 200. Polyethylene glycol monomethyl ether of a hydrophilic section initiates ring-opening polymerization between diselenium macrocyclic carbonate andtrimethylene carbonate to obtain polydiselenium carbonate. The polymer can serve as an anti-tumor medicine. The polydiselenium carbonate is controllable in structure, selenium content and anti-tumoractivity are adjustable, polymer nano-particles directly serve as medicines to be used, and the polymer is single in component and simple to prepare and avoids the problems of poor stability, complicated process and the like when the medicines are entrapped by common medicine carriers.

The invention discloses a quinazoline derivative shown in formula (I) which is described in the specification and a salt thereof. In the formula, Z represents -NH- and -O-, R1 and R2 represent C1-3 alkoxy groups or hydrogen, R3 is selected from the group consisting of 4-fluoro-, 4-chloro-, 2-chloro-, 4-bromo-, 2, 4-dichloro-, 4-methyl, 4-methoxy, hydrogen, 4-trifluoromethyl and 2,4-dimethoxy. The invention relates to a preparation method and application of the compound shown in the formula (I) and the salt thereof. The compound or the salt thereof has strong inhibitory activity on colorectal cancer cell strains HCT-116, human lung cancer cell strains A549 and breast cancer cell strains MCF-7. The compound has wide spectrum antitumor activity and can be used as a drug or lead compound for treatment of diseases like tumors and cancers.

The invention relates to garcinia acid amide derivative and preparation method thereof and purpose, and the structural formula of the derivative is shown as formula (I); The preparation method comprises the following steps: garcinia acid and nucleoside medicament or salt nucleoside of nucleoside medicament melted in an inertia solvent under room temperature; then a catalyzed condensation reagent is added for reaction for 3 to 5 hours by blending at the temperature between 40 and 60 DEG C; and garcinia acid amide derivative is obtained after washing, drying, distillation andn column chromatography. The derivative of the present invention can be used for used to prepare compositions, antineoplastic drugs, antimycotics drugs or anti-angiogenic drugs generation medicament or be used with other anticancer active components. The compound of the present invention not only displays better activity to a plurality of tumor cells, shows good targeting to tumor cells, which makes a good foundation for novel medicament exploitation.

Disclosed are compounds represented by formula (I), pharmaceutically acceptable salts thereof, solvates thereof, and solvates of the pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, W and are as defined in the present application.

A multi drug resistance of the lung cancer cell line relates to a multi drug resistance cell line. The invention is to analyze the morphology and biological ethology change of tumour cells after chemotherapy drug resistance, screen the chemotherapy drugs and decide the sensitivity of the chemotherapy drugs, analyze the multi drug resistance mechanism of tumour chemotherapy and screen multidrug resistance reversal agents in vitro, which provides a multi drug resistance of the lung cancer cell line. The establish of the multi drug resistance of the lung cancer cell line includes: (1) placing the Anip973 cells into culture solution containing foetal bovine serum, penicillin and streptomycin and laying them in a environment with a temperature of 37 DEG C and 5% of carbon dioxide concentration; (2) when the Anip973 cells cover 70%-90% of the incubator inwall area, continuing to culture the Anip973 cells in NVB solution with 0.01-0.02 mug / mL for 24h; (3) throwing the NVB solution and adding culture solution with the same volumes, after the generation of the survival Anip973 cells then entering the logarithmic growth phase, continuing to culture for 24h in NVB solution with an increased concentration; (4) repeating the step (3) until the concentration of NVB reach 2.0-2.2 mug / mL, then the Anip973 / NVB cell line is prepared.

The invention belongs to the field of medicinal chemistry, and relates to a class of isonicotinic acid derivatives with novel structures, a preparation method and application thereof. The present invention mainly relates to isonicotinic acid derivatives represented by formula (I), stereoisomers, racemates, tautomers, or pharmaceutically acceptable salts thereof, and preparation methods thereof and in the preparation of anticancer Uses in medicine. In formula (I): Z is selected from O, S, NR 3 , where R 3 for hydrogen or C 1 ~C 6 the alkyl group; R 1 from C 1 ~C 6 Alkyl, C 1 ~C 6 Alkoxy, halo C 1 ~C 6 Alkyl, aryl, aryloxy, heteroaryl, heteroaryloxy, heterocyclyl, heterocyclyloxy, halogen; R 2 selected from halogen, cyano, nitro, C 1 ~C 6 Alkyl, C 1 ~C 6 Alkoxy or halo C 1 ~C 6 Alkyl; m is an integer of 0-4; n is an integer of 0-5; with the proviso that Z is selected from NR 3 , when m is 0 and n is 1, R 2 Not halogen.

The invention discloses a sulfonyl ester anthraquinone derivative, a preparation method and application thereof. The sulfonyl ester anthraquinone derivatives of the present invention have good anti-tumor activity, and the half maximal inhibitory concentrations to Hela, MCF-7, A549, CNE2 and other cell lines are all less than 100 μmol / mL, and have no inhibitory effect on normal cells. The invention introduces a sulfonyl ester group on the anthraquinone core to improve its water solubility and acidity and alkalinity, so as to improve the antitumor activity of the anthraquinone compound, and the preparation method is simple and feasible. The sulfonyl ester anthraquinone derivatives of the invention have wide potential applications in fluorescent materials, medicine, pesticides, materials and the like, especially in the preparation of anticancer drugs.

The invention belongs to the field of medicinal chemistry, and in particular relates to a class of novel pyridine-2-carboxylic acid derivatives and their preparation method and application. The present invention mainly relates to pyridine-2-carboxylic acid derivatives shown in the following formula (I), their stereoisomers, racemates, tautomers, or pharmaceutically acceptable salts thereof, and their preparation methods and Use in the preparation of anticancer drugs.