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

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 a seven-membered-ring berberine analogue and a pharmaceutically acceptable salt thereof. Particularly, the analogue has a structure in a formula A, wherein definitions of all substituent groups are described in the description. The invention further provides a preparation method of the seven-membered-ring berberine analogue as shown in the formula A and application of the seven-membered-ring berberine analogue in preparing drugs for preventing or treating tumors or cancers. Please see the formula in the description.

The invention relates to the technical field of medicines, in particular to an NAMPT protein degradation targeted chimera. The NAMPT protein degradation targeted chimera is a compound as shown in a general formula (i) and / or (ii) or pharmaceutically acceptable salt thereof. The invention also relates to a preparation method and application of the NAMPT protein degradation targeted chimera. The compound shows the good NAMPT enzyme inhibition activity, can down-regulate the intracellular and extracellular NAMPT protein levels in a ubiquitin proteasome way to realize tumor inhibition, has the certain broad-spectrum antitumor activity, can obviously inhibit tumor growth, and can be applied to NAMPT mediated tumor diseases.

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 present invention relates to a gambogic acid derivative, a preparation method and uses thereof. The structure formula of the derivative is represented by a formula (I). The preparation method comprises: in an inert solvent, carrying out a reaction of gambogic acid and p-aminomethyl benzoate (formula (III)) or chloromethyl benzoate. The gambogic acid derivative can be used for preparing compositions, anti-tumor drugs, antifungal drugs or anti-angiogenesis drugs, or combining with other anti-cancer active ingredients to be used. In addition, the gambogic acid derivative provides good activity for plural types of tumor cells, and presents good tumor cell targeting performances so as to establish a foundation for development of novel drugs.

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.

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 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 is a platinum complex formula (I) wherein X represents a halogen atom, B represents, independently to each other, a halogen atom, a hydroxyl group or a carboxylate group containing 1 to 6 carbon atoms, and A represents a primary tricyclic amine containing 10 to 14 carbon atoms which may be optionally substituted on the tricyclic ring by one or two alkyl group(s) each containing 1 to 4 carbon atoms, and, furthermore, an inclusion complex of the above platinum complex with beta- or gamma-cyclodextrin which may be optionally substituted by hydroxyalkyl groups containing 1 to 6 carbon atoms. There is also disclosed a process for the manufacture of the complex of formula (I) based on oxidation of a complex of divalent platinum of formula (II) with hydrogen peroxide and on optional substitution of hydroxyl groups in the obtained product with carboxylate groups by action of an acylating agent. The disclosed complexes may be used as such or as a part of pharmaceutical composition in a therapy of oncologic diseases.

The invention belongs to the field of medicinal chemistry, and particularly relates to a pyridine-2-formic acid derivative of a novel structure and a preparation method and application thereof, in particular to the pyridine-2-formic acid derivative represented by formula (I), a stereoisomer, racemate, tautomer or pharmaceutically acceptable salt of the pyridine-2-formic acid derivative, a preparation thereof of the pyridine-2-formic acid derivative and the application of the pyridine-2-formic acid derivative in preparing anti-cancer drugs.

The invention relates to an epirubicin (EPI) derivative with anticancer activity, in particular to a compound shown as a formula (I) and salts or solvates thereof, a preparation method of the compound shown as the formula (I) and application of the compound serving as medicinal active ingredients. The epirubicin derivative provided by the invention has the equivalent activity and even higher than that of the epirubicin in a cellular level. The formula (I) is shown in the description.

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 sulfonyl ester group anthraquinone derivative, a preparation method and application thereof. The sulfonyl ester group anthraquinone derivative provided by the invention has good anti-tumor activity, has a median inhibitory concentration of less than 100micromol / mL on Hela, MCF-7, A549, CNE2 and other cell lines, and has no inhibition on normal cells. According to the invention, sulfonyl ester group is introduced to an anthraquinone parent nucleus to improve the water solubility and acidity and acid-base properties so as to improve the anti-tumor activity of anthraquinone compounds, and the preparation method is simple and feasible. The sulfonyl ester group anthraquinone derivative provided by the invention has wide potential applications in fluorescent materials,medicine, pesticides, materials, etc., and especially has application value in preparation of anticancer drugs.

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 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 discloses a 2-trifluoromethyl-4-aminoquinazoline compound and application thereof, and the compound has a structural formula as shown in the following general formula I. According to the invention, trifluoromethyl is introduced to a 2-site of a 4-aminoquinazoline compound, and 4-amino is modified, so that the 2-trifluoromethyl-4-aminoquinazoline compound is obtained. A series of 2-trifluoromethyl-4-aminoquinazoline derivatives with novel structures are designed and synthesized by taking 2-trifluoromethyl-4-aminoquinazoline as a raw material, the probability of interaction between the compound and a target is increased, the biological activity and chemical stability of the compound are improved, and the druggability of the compound is improved, so that the 2-trifluoromethyl-4-aminoquinazoline compound has efficient and broad-spectrum anti-tumor activity.

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 and their preparation methods and uses. The present invention mainly relates to isonicotinic acid derivatives, stereoisomers, racemates, tautomers, or pharmaceutically acceptable salts thereof represented by formula (I), their preparation methods, and their use in the preparation of anticancer drugs. Uses in medicines. In formula (I): Z is selected from O, S, NR 3 , where R 3 is hydrogen or C 1 ~C 6 Alkyl; R 1 Selected from C 1 ~C 6 Alkyl, C 1 ~C 6 Alkoxy, haloC 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 haloC 1 ~C 6 Alkyl; m is an integer from 0-4; n is an integer from 0-5; provided that Z is selected from NR 3 , when m is 0 and n is 1, R 2 Not halogenated.

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.