195results 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 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 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.

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 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 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 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 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 present invention provides heterocyclic compounds as selective inhibitors of fibroblast growth factor receptor 4 (FGFR4), pharmaceutical compositions containing the compounds, methods of preparingthe compounds, and methods of treating cell proliferative diseases, such as cancer, using the compounds of the invention.