197results about How to "Strong antiproliferative activity" patented technology

In a cytotoxic compound of the general formula (I) R is H or methyl or methylene substituted by C1-C4 straight or branched alkyl, R1 is selected from the group consisting of H, C1-C4 straight or branched alkyl, methoxy, methoxy substituted by from one to three fluorine, halogen; R2 is H or C1-C4 straight or branched alkyl; X is CH or N; Y is CH or N.

The invention discloses two halogenated 8-hydroxyquinoline platinum (II) complexes and a synthesis method and application thereof. The structures of the halogenated 8-hydroxyquinoline platinum (II) complexes are shown in the formula (I), and the synthesis method comprises the steps that an 8-hydroxyquinoline derivative and dichloro bis(dimethyl sulfoxide) platinum are taken and subjected to a coordination reaction in a polar solvent, and the halogenated 8-hydroxyquinoline platinum (II) complexes are obtained. It is shown through experiments carried out by an applicant that the halogenated 8-hydroxyquinoline platinum (II) complexes have good activity of inhibiting the proliferation of certain tumor cell strains and can selectively inhibit the growth of bladder cancer T-24 cells, and the apoptosis of the tumor cells is induced under the function of targetedly interfering with mitochondria; meanwhile, the toxicity of the complexes to human normal cells HL-7702 is low. The structures of the halogenated 8-hydroxyquinoline platinum (II) complexes and the structure of the 8-hydroxyquinoline derivative are shown in the following formulas (I) and (II) respectively, wherein the formulas (I)and (II) are shown in the description, and R1 represents Cl or Br.

The invention relates to quinazolinyl-aryl urea derivatives with antitumor function disclosed as general formula (II) and application thereof. The substituent group in the general formula (II) is defined in the specification. By using sorafenib and gefitinib as lead compounds, the pharmacophore-uramido group of the sorafenib is retained; and meanwhile, the quinazoline rings in the gefitinib and other EGFR-TKIs are retained to synthesize a series of quinazolinyl-aryl urea derivatives. The in-vitro activity test proves that parts of the compounds have excellent antitumor activity, and the compounds have higher research and practical values. (II).

The invention belongs to the field of medical technology and relates to preparation and application of a series of curcumin analogues. The curcumin analogues have structures as shown in the formula I, formula II and formula III, wherein R, R1 and R2 are as mentioned in the specification. Pharmaceutically acceptable salt and solvate of the curcumin analogues and a medicine containing the curcumin analogues or the pharmaceutically acceptable salt used as active components can be used in treatment of cancer. The curcumin analogues and the pharmaceutically acceptable salt have a good anticancer activity. A preparation method of the curcumin analogues is simple and feasible and is easy to operate.

The invention discloses a 7-substituted-4-aryl coumarins compound, and a preparation method and an application thereof and belongs to the technical field of antitumor drugs. The 7-substituted-4-aryl coumarins compound is acquired in the manner of modifying and remolding 4 and 7 loci of the coumarins. The structural formula is shown in the specification. A pharmacological experiment proves that such a compound has an excellent antitumor activity, can be used for preparing the antitumor drugs, is capable of supplying a new selection for the development and application of the antitumor drugs and further can be applied to the design and optimization of the antitumor drugs. The preparation method of the compound has the advantages of easily acquired raw materials, mild reaction condition, easily realized synthesis method, simple reaction process and operation, low-cost reagents and higher yield.

The invention relates to the field of pharmaceutical chemistry, in particular relates to a histone deacetylase inhibitor (I) containing an alpha amino acid structure and a preparation method thereof. The invention also discloses an intermediate (V). Ar, R1, L1, L2 and A are defined in the specification. A pharmacological experiment proves that the compound in the invention has a good inhibition effect on histone deacetylase, exhibits obvious selectivity on Class IHDACs, and has a good antiproliferative activity on tumor cell strains.

The invention relates to a polysubstituted isoindoline compound represented by a general formula (I), and a preparation method, a pharmaceutical composition and an application thereof. Specifically, as a CRL4CRBNE3 ubiquitin ligase regulator with a novel structure, the polysubstituted isoindoline compound provided by the invention has stronger anti-tumor activity and an anti-tumor spectrum, and can be used for preparing medicines for treating diseases related to CRL4CRBNE3 ubiquitin ligase.

The invention provides a preparation method and applications of a 4-phenoxy phenyl pyrazolo pyrimidine amide derivative. The compound has a structure represented by a formula (I), wherein X and Y aretwo linking groups, X is selected from benzyl, substituted benzyl, piperidyl and C1-6 straight-chain or branched-chain alkyl, Y is -(CH2)n-, n is any integer selected from 0-4, R is selected from hydroxyl, hydroxyamino and o-phenylenediamine, and the structure of the formula (I) comprises a racemate and a stereoisomer. The compound has a BTK / HDAC double-target inhibition effect and growth inhibition activity on T cell leukemia cells and mantle cell lymphoma cells, and is used for preparing antitumor drugs.

The invention belongs to the technical field of medicines, and particularly relates to a pyridopyrimidine KRAS G12C mutant protein inhibitor shown in a general formula (I), pharmaceutically acceptable salts, stereoisomers and deuterated substances thereof. The invention also relates to a preparation method of the compounds, and a preparation method of the pharmaceutically acceptable salts, pharmaceutical preparations and pharmaceutical compositions containing the compounds. The invention also relates to the application of the compounds, pharmaceutically acceptable salts containing the compounds, pharmaceutical preparations and pharmaceutical compositions of the compounds in treatment of cancer proliferative diseases caused by KRAS G12C mutant protein.

The invention discloses a benzotriazole small-molecule compound shown in structural formula (1) or pharmaceutically acceptable acid added salt of the compound and pharmaceutical composition containing the compound. The invention further discloses a medical application of the benzotriazole small-molecule compound or the pharmaceutically acceptable acid added salt of the compound to preparation of drugs for treating growth, transfer and recurrence of diseases such as various malignant tumors caused by RAS gene mutation.

The invention discloses a Cucurbita moschata protein 2 and a preparation method and application thereof, which relates to the field of biochemistry. The invention discloses a new ribosome inactivated protein extracted from flesh of Cucurbita moschata, namely the Cucurbita moschata protein 2 (type 2 Cucurbita moschata ribosome inactivated protein cucurmosin 2). The molecular weight of the Cucurbita moschata protein 2 is determined as 2, 7183Da by ESI-MS. The Cucurbita moschata protein 2 is put into phosphate buffer, citric acid buffer and Tris-HCl buffer in advance, and a single crystal for the diffraction of X-ray is produced taking carbowax as a precipitator. Through preliminary analysis, the crystal structure shows that the crystal is a type 1 ribosome inactivated protein with the functions of tumor and virus resistance, in particular human immunodeficiency virus resistance, thereby laying a material foundation for obtaining a protein for medicine use or preparing immunotoxin.

Novel CUR- and CUR-BF2 compounds exhibiting anti-tumor properties are presented. CUR compounds bearing fluorinated moieties with selective fluorine introduction into the α-carbonyl moiety as well as CUR-BF2 adducts and CURs with diverse substitution patterns in the phenyl rings including fluorinated substituents (SCF3, OCF3, and F) and / or bulky activating groups (OMe, OAc, and OBz) are presented. Fluorinated aryl-pyrazoles and isoxazoles as well as novel CUR and CUR-BF2 compounds with monocyclic aromatic and bicyclic-heteroaromatic lateral rings, bearing fluorine(s), OCF3, CF3, and SCF3 groups, and their alpha-carbonyl-fluorinated analogs, as well as their pyrazole and isoxazole derivatives are presented. The CUR-pyrazoles embody analogs that are fluorinated at the phenyl-pyrazole moiety. The compounds and their derivatives exhibited exceptional cytotoxic and anti-proliferative activity against several cancer cell-lines. Deuterated CUR-BF2 and CUR compounds were also synthesized.

The invention relates to a pyrazolo[1,5-a]miazine compound and its preparation method and medical use. The invention relates to the preparation method of the pyrazolo[1,5-a]miazine compound shown in the general formula (I) and its salt, a pharmaceutical composition containing the pyrazolo[1,5-a]miazine compound or its medicinal salt, the use of the pyrazolo[1,5-a]miazine compound or the pharmaceutical composition in the medicine field and especially as a receptor tyrosine kinase inhibitor and a c-Met inhibitor, and the use of the pyrazolo[1,5-a]miazine compound or the pharmaceutical composition in preparation of drugs for preventing and / or treating c-Met abnormality-related diseases.

The invention relates to glucose derivatives of glaucocalyxin A. The glucose derivatives have a structure represented by a formula I or a formula II, wherein R1 represents hydrogen or methoxyl, R2 represents hydrogen or acetyl, and n represents 0 or 1. The invention further relates to a preparation method and application of the glucose derivatives. By virtue of a cytotoxic activity evaluation experiment, a result shows that the glucose derivatives of glaucocalyxin A have relatively strong inhibitory activity for human tumor cell proliferation, and the activity is superior to that of a parent compound, namely glaucocalyxin A. (The formula is shown in the description).

The invention belongs to the technical field of medicinal chemistry and pharmacology, and relates to a diphyllin ether derivative and a preparation method and application thereof. The chemical structural formula of the diphyllin ether derivative is shown as a formula (I), the diphyllin ether derivative is prepared by reacting diphyllin with anhydrous potassium carbonate and epoxy bromopropane in N, N '-dimethylformamide to obtain 4-O-epoxypropyl diphyllin, and then reacting the 4-O-epoxypropyl diphyllin with a corresponding amine compound or a nitrogen-containing heterocyclic compound in methanol. The diphyllin ether derivative has high activity of inhibiting tumor cell growth and can be expected to be used as an antitumor drug.

The present invention belongs to the field of natural medicines and discloses a compound medicine composition with anti lymphoma activity containing piperlongumine and houttugnin and use thereof. Active ingredients of the compound medicine composition comprise the piperlongumine and the houttugnin in a molar ratio of 1:1 to 1:20. Through combination of the piperlongumine and the houttugnin, the compound medicine composition has a strong synergistic treatment effect on lymphoma.

The invention discloses a histone deacetylase subtype inhibitor, namely a thioacetyl arylamine compound and application thereof. Pharmacological experiments show that the compound has a selective inhibition effect on HDAC6 enzyme, shows high anti-proliferative activity on various tumor cells, and is low in toxicity to normal cells and low in potential cardiotoxicity. Moreover, the compound has a protective effect on nerve cells, is ideal in pharmacokinetic characteristics, and has relatively high blood-brain barrier dredging characteristics. The compound disclosed by the invention has a deep development prospect as a high-efficiency low-toxicity anti-tumor or neurodegenerative disease therapeutic agent. The structural general formula of the histone deacetylase subtype inhibitor, namely thethioacetyl arylamine compound is as shown in the specification.

The invention discloses a 3,4-disubstituted pyrrole compound. The compound has the following structure shown in a general formula in the specification. A preparation method of the 3,4-disubstituted pyrrole compound comprises a step of performing Michael addition, cyclization and elimination reaction on disubstituted olefin and p-toluenesulfonyl isocyanide. Compared with the prior art, a series of 3,4-disubstituted pyrrole compounds disclosed by the invention have high antitumor activity in vitro; meanwhile, the proliferation inhibition activity to normal cells is inhibited weakly, the excellent tumor cell selectivity is displayed, and the 3,4-disubstituted pyrrole compound can be used as a kind of safe and effective antitumor drugs in the future. The preparation method is convenient to carry out, short in reaction period and high in yield.

The invention belongs to the field of natural medicine, and discloses a compound medicine composition with a lung cancer resistant effect and application of the compound medicine composition. Active ingredients of the compound medicine composition consist of piperlongumine and rheum emodin in a molar ratio of (1:1) to (1:10). By combining the piperlongumine and rheum emodin, a synergic effect for treating the lung cancer is relatively good.

The invention relates to a podophyllotoxin-retinoic acid heterocomplex synthesis method and application of a podophyllotoxin-retinoic acid heterocomplex in a medicine for preventing and curing tumors. The podophyllotoxin-retinoic acid heterocomplex has a structural formula as shown in a formula I (shown in the description); a preparation method of the compound as shown in the formula (I) is as follows (shown in the description), wherein a to b represent reaction conditions: a: a reagent is oxalyl chloride, a solvent is methylbenzene, and reaction temperature is 20 to 35 DEG C; b: a solvent is dichloromethane, a catalyst is triethylamine, and reaction temperature is 10 to 30 DEG C. A solvate is a complex prepared from the compound as shown in the formula (I), ethyl alcohol, diethyl ether, n-butyl alcohol, water, acetone or an isopropanol solvent. An experimental result shows that the podophyllotoxin-retinoic acid heterocomplex has a strong inhibiting effect on two human gastric cancer cell strains, and has an IC50 value in a nano-mole level, which is remarkably better than that of positive control agents: retinoic acid and etoposide. The compound as shown in the general formula (I) has the highest antiproliferative activity on human gastric cancer BGC-823 cells, is used for preventing and curing cell proliferation abnormity related diseases, and is particularly applied in the medicine for preventing or curing the tumors.

The invention discloses preparation and application of an aminopyrimidine derivative selectively targeting CDK9, in particular, a preparation method of the compound and application of the compound in prevention and / or treatment of tumor-related diseases including glioma, various leukemia, lymphoma, liver cancer, stomach cancer, prostate cancer, ovarian cancer, breast cancer, lung cancer and the like. The compound can effectively and selectively inhibit the activity of CDK9 protein, and meanwhile, the compound shows remarkable anti-tumor activity in cancer cells such as MV4-11, MCF-7 and MOLM-13.

The invention discloses an aromatic heterocyclic lactam compound as well as a preparation method and an application thereof. The invention particularly discloses an aromatic heterocyclic lactam compound shown as a formula (I), or pharmaceutically acceptable salt thereof, or an enantiomer, a diastereoisomer, a tautomer, a solvate, a polymorphic substance or a prodrug thereof, a preparation method of the aromatic heterocyclic lactam compound and an application of the aromatic heterocyclic lactam compound to pharmacy.

Among antibodies exhibiting reactivity to natural TGF[alpha], antibodies having low reactivity to G79A-substituted TGF[alpha] are identified as exhibiting superior antiproliferative activity against cancer cells having a mutation in the Ras gene. Further identified is that many of the antibodies also inhibit the tyrosine phosphorylation of EGFR and / or inhibit the induction of vascular endothelial cells.

The invention belongs to the technical field of medicinal chemistry and pharmacology, and relates to a diphyllin heterocyclic derivative as well as a preparation method and application thereof. The diphyllin heterocyclic derivative has a chemical structural formula shown as a formula (I), is of a non-glucoside structure and has metabolic stability superior to that of glucoside compounds. These derivatives are found to have strong activity of inhibiting tumor cell growth, and can be expected to be used as antitumor drugs.

The invention discloses an artemisinin derivative, a synthesis method and applications thereof. The artemisinin derivate is N-(3-N',N'-dimethylamino-propyl)-10-azadeoxyartemisinin, which is prepared by reacting artemisinin with N,N-dimethyl-1,3-diaminopropane and p-toluene sulfonic acid in sequence. By researching the proliferation inhibition activity of the derivative on multiple human tumor cell strains and human normal cell strains, the applicant finds that the derivative has a prominent proliferation inhibition activity on human bladder cancer cell T-24, human ovarian cancer cell SK-OV-3, and human stomach cancer cell MGC80-3, has a potential medicinal value, and can be used to prepare various antitumor drugs.

The invention relates to a 5-benzylidene-2-phenyl thiazolone compound as well as preparation and application thereof. In particular, the compound provided by the invention has a structure shown as a general formula (I), wherein the definitions of each group and substituent are described in the description. The invention further discloses a preparation method of the compound and application of thecompound to the prevention and / or treatment of cancer-related diseases. The compound provided by the invention has superior inhibitory activity on protein-arginine methyltransferases 1 (PRMT1), protein-arginine methyltransferases 5 (PRMT5) and histone demethylase LSD1, and can induce tumor cell apoptosis and retard tumor cells at a G1 stage, so that the compound can be used for preparing a seriesof medicaments for treating diseases related to abnormal activities of the PRMT1, the PRMT5 and the histone demethylase LSD1. The general formula (I) is shown in the description.

The invention discloses a compound medicine composite with a breast cancer resistance function, application of the composite and medicine based on the composite. The active content of the compound medicine composite is composed of doxorubicin and piperlongumine with the mole ratio of 1:5-1:15. According to an experiment, an MDA-MB-231 human breast cancer cell is used as a model, and through an MTTexperiment, by applying CompuSyn software analysis, it is discovered that a good synergistic effect is achieved during compatibility of doxorubicin and piperlongumine with the mole ratio of 1:10; through a cell apoptosis experiment, it is discovered that the apoptosis-promoting effect is obviously superior that that of a single medicine group when the two kinds of medicines cooperate for use; through a naked mouse cancer-bearing medicine application experiment, it is discovered that growth of heterograft tumors of MDA-MB-231 cells in the naked mouse can be effectively inhibited through a medicine cooperation application group, and the effect of the medicine cooperation application group is obviously superior that that of the single medicine group. In this way, medicine cooperation application of doxorubicin and piperlongumine has the high function of inhibiting the breast cancer through cooperation, and accordingly the composite has good clinical medicine application development prospects.

The invention provides a GnRH analogs-antineoplastic drug conjugate. The structure of the conjugate is GnRHa-Linker-Dox. The GnRHa is a GnRH analogue. The Linker is a connecting arm and is used for coupling the GnRHa with an antineoplastic drug. The Dox is an antineoplastic drug doxorubicin. The invention further provides a preparation method of the GnRH analogs-antineoplastic drug conjugate and application to drugs for the prevention or treatment of tumors of the GnRH analogs-antineoplastic drug conjugate. The conjugate has good tumor cell selectivity, can target tumor cells which over-express GnRH receptors, and the toxic side effects of the doxorubicin are reduced. The The conjugate lays a foundation for research and development of a new type of anti-tumor drug targeting GnRH receptors,and good application prospects are achieved.

The invention discloses an application of Aspeverin in preparation of medicines for inhibiting liver fibroblast proliferation. Pharmacological testing proves that the Aspeverin can obviously inhibit liver fibrosis from being caused and developed, and can be used for preparing the medicines for resisting liver fibrosis and treating liver cirrhosis. The application of Aspeverin in preparation of medicines for inhibiting liver fibroblast proliferation is disclosed for the first time, a framework type belongs to a brand-new framework type, the Aspeverin has an unexpected strong effect of inhibiting the liver fibroblast proliferation activity, and the revelation possibility of other compounds cannot be generated, so that the application has obvious substantive features; and moreover, the application has an obvious improved effect of inhibiting the liver fibroblast proliferation.

The invention discloses synthetic peptide sp2 and application thereof. The amino acid sequence of the sp2 is shown by SEQ ID NO.1. The efficacy characteristics are that the synthetic peptide sp2 has obvious activity of resisting tumor growth against xenograft tumor such as nude-mouse subcutaneous human pancreatic cancer, human cervical cancer and human ovarian cancer in dose-effect and time-effectrelationships, and realizes the functions of delaying transfer and prolonging the lifetime for the nude-mouse orthotopic transplantation human pancreatic cancer and lung adenocarcinoma. The safety characteristic is that toxic reaction or death does not occur after 2,000 mg / kg BW of sp2 is applied to an animal through intravenous injection. The sp2 is also applied to: (1) the prevention and / or treatment of tumor; (2) inhibition of the proliferation and / or growth and / or invasion of tumor cells; (3) enhancement of anti-tumor immunoreaction; (4) induction of tumor cell differentiation; (5) preparation of class-A anti-tumor drugs; (6) inhibition of tumor telomerase activity; (7) control of tumor cell cycle; (8) preparation of products for regulating and controlling tumor cell cycle.