148 results about "Tubulin polymerization" patented technology

A serious of nitro heterocyclic derivatives including a structure of formula (I) are provided. In formula (I), P, Q and R1 to R8 are defined in the specification. The derivatives disclosed in the present invention are characterized in inhibiting tubulin polymerization, and treating cancers and other tubulin polymerization-related disorders with a suitable pharmaceutical acceptable carrier.

Indole derivatives and analogous compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat cancer, metastatic cancer, resistant cancer or multidrug resistant cancer, including inter-alia: prostate cancer, breast cancer, melanoma, colon cancer and bladder cancer.

The invention relates to a catalyst component used for olefin polymerization and a preparation method thereof as well as a catalyst used for olefin polymerization and application. The catalyst component comprises reaction products of the following components: (1) a solid component and (2) at least one titanium compound, wherein the solid component comprises a magnesium compound shown in Formula (1) (shown in the description) and epoxy alkanes compounds shown in Formula (2) (shown in the description); R1 is linear alkyls or branched alkyls with C1-C12; R2 is the same as or different from R3; R2 and R3 are hydrogen, or linear alkyls or branched alkyls with C1-C5 independently; hydrogen on alkyls is optionally replaced by halogen; X is halogen, m ranges from 0.1 to 1.9, n ranges from 0.1 to 1.9, and m plus n is equal to 2. By adopting the catalyst component in the process of olefin polymerization, relatively high polymerization activity and relatively high stereotactic capability can be acquired.

The antifungal and cancer cell growth inhibitory activities of 1-(3′,4′,5′-trimethoxyphenyl)-2-nitro-ethylene (TMPN) were examined. TMPN was fungicidal for the majority of 132 reference strains and clinical isolates tested, including those resistant to fluconazole, ketoconazole, amphotericin B or flucytosine. Minimum fungicidal concentration/minimum inhibitory concentration (MFC/MIC) ratios were ≦2 for 96% of Cryptococcus neoformans clinical isolates and 71% of Candida albicans clinical isolates. TMPN was fungicidal for a variety of other basidiomycetes, endomycetes and hyphomycetes, and its activity was unaffected by alterations in media pH. TMPN was slightly cytotoxic for murine and human cancer cell lines (GI₅₀=1-4 μg/ml), and weakly inhibited mammalian tubulin polymerization (IC₅₀=0.60 μg/ml). TMPN may also be used as a biochemical probe for tubulin and fungal dimorphism studies.

Indole derivatives and analog compounds and pharmaceutical compositions comprising the same are provided. Also provided are methods of using these compounds to inhibit tubulin polymerization in a cell associated with a proliferative disease or to treat a cancer.

The invention discloses perylene diimide-based photoelectric functional materials and a preparation method thereof. A series of polymers with different contents are prepared through Suzuki polymerization, Yamamoto polymerization, Stille polymerization or Sonogashira polymerization. The materials have good thermal, photic and chemical stability and good application prospects in the fields such as organic solar cells and the like. The structural formula of the perylene diimide-based polymers is shown in the specification, wherein a is a number between 1 and 30; b is a number between 0 and 30; R is C1-C10 alkyl or alkoxy; A1 is any one of the following structures shown in the specification, wherein n is a number between 1 and 10; and R is C1-C10 alkyl.

The invention provides a catalyst component, a catalyst and a method for olefin polymerization. An internal donor a and an internal donor b are used as internal donors, so that when the catalyst component and the catalyst are used for olefin polymerization, the catalyst component and the catalyst have high stereo selectivity, high activity and high hydrogen response, and the prepared olefin polymer has wide molecular weight distribution, wherein the internal donor a is a compound shown as a formula (I); and in the formula (I), R1 and R3 are same or different, and refer to a straight-chain or branched-chain alkyl with the carbon atom number of 1-10, naphthenic base with the carbon atom number of 3-10 or substituted or non-substituted aryl with the carbon atom number of 6-20; R2 refers to straight-chain or branched-chain alkylene with the carbon atom number of 1-6 and substituted or non-substituted aryl with the carbon atom number of 6-20; and n is an integer from 2 to 10.

The invention relates to compounds of structural formula (I):

• • or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein R_a, R_b, and R₂ are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

Trimethoxyphenyl substituted indole ligands have been discovered which demonstrate impressive cytotoxicity as well as a remarkable ability to inhibit tubulin polymerization. Such compounds as well as related derivatives are excellent clinical candidates for the treatment of cancer in humans. In addition, certain of these ligands, as pro-drugs, may well prove to be tumor selective vascular targeting chemotherapeutic agents or to have vascular targeting activity resulting in the selective prevention and/or destruction of nonmalignant proliferating vasculature.

The invention relates to compounds of structural formula (I):

or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein R_a, R_b, and R₂ are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.

The invention discloses a novel phenoxy ester coordinated transition metal organic complex, an olefin polymerization catalytic system comprising the same and an application of the catalytic system. The catalytic system comprises (A) a transition metal organic complex with a general formula (I) and (B) main group metal organic compounds, organic aluminoxane and ionic compounds which can be ionized. The transition metal organic complex is shown in the general formula (I), wherein in the formula, M is one or more of transition metal elements in an IV, V or VIII subgroup in the periodic table of elements, m is an integer from 1 to 3, n is a number satisfying the M valence state, X is halogen, alkoxy and the like, R1 is C1-20 alkyl or C6-20 aryl or substituted aryl, and R2-R5 are the same or different and are selected from hydrogen atoms, halogen atoms, alkyl, silyl and the like. The catalytic system has the advantages of high catalytic activity, good thermal stability, strong copolymerization capability and the like, can catalyze olefin polymerization and copolymerization, and can be used in various polymerization methods.

A chain transfer agent composition comprises at least one branched C₁₀ mercaptan selected from 5-methyl-1-mercapto-nonane, 3-propyl-1-mercapto-heptane, 4-ethyl-1-mercapto-octane, 2-butyl-1-mercapto-hexane, 5-methyl-2-mercapto-nonane, 3-propyl-2-mercapto-heptane, 4-ethyl-2-mercapto-octane, 5-methyl-5-mercapto-nonane, or combinations thereof. The chain transfer agent composition can be a component of an emulsion polymerization mixture and can be used in a process for emulsion polymerization for the production of polymers, for example, via free-radical polymerization.

Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof:

R²—Y—Z-Q-A-R¹  Formula (I)

wherein R¹, R², Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.

The invention relates to the technical field of drugs, in particular to application of quinazoline compounds. The invention discloses application of the quinazoline compounds shown in the general formula I or pharmaceutically acceptable salt, prodrugs or isomers thereof in preparing mitotic inhibitors. The quinazoline compounds shown in the general formula I or pharmaceutically acceptable salt, prodrugs or isomers have the effect of inhibiting tubulin polymerization and can effectively inhibit mitosis.

The invention provides a gamma-carboline derivative, which is obtained by using gamma-carboline with antineoplastic activity as a lead compound, and introducing different lateral chains, aromatic rings, aromatic heterocycles or heterocycles to the sixth position of the gamma-carboline. Pharmacological active screening test shows that the compound has in-vitro antihyperplasia function on tumor cells; partial compound has obvious anti-tumor activity; the value of IC50 reaches mu M grade to show cytotoxicity similar to positive control polyenic taxusol; and significant microtubulin polymerization retardation activity and DNA intercalation function are presented in primary activity mechanism research; therefore, the compound is expected to be a new antineoplastic reagent with double functions of micromolecular microtubulin and DNA. The gamma-carboline derivative has the advantages of reasonable design, wide source of raw materials, easy preparation, mild reaction condition, simple operation and practicality. The structural formula of the compound is shown as the above.

The invention discloses 3, 4-dihydroisoquinoline antitumor compounds, a preparation method of the compounds, and an application of the compounds in preparation of antitumor medicines. The compounds have a structural formula (I) as shown in the specification. The compounds disclosed by the invention are structurally novel antitumor compounds which have the double mechanisms of inhibiting kinase VEGFR-2 (Vascular Endothelial Growth Factor Receptor-2) and promoting tubulin polymerization, and have good antitumor activity.

The invention discloses a two-alkoxyl-silicon-containing alpha-diimine compound and the application of a load type metal complex thereof in olefin polymerization. The alpha-diimine compound structurecontains two active groups, namely alkoxyl silicon, so that the alpha-diimine compound can be loaded on the surface of a carrier in a covalent grafting manner; moreover, the two active groups greatlyincrease the firmness of the alpha-diimine compound loaded on the carrier. The loaded alpha-diimine compound is matched with the metal complex to obtain an alpha-diimine compound-loaded metal complexwhich is applied to the olefin polymerization. During the olefin polymerization, the loaded metal complex used as a catalyst is high in thermal stability and can still keep relatively high activity ata reaction temperature of 100 DEG C; the catalyst is hard to fall off, and the phenomenon of kettle sticking during the polymerization is obviously improved.

The invention is concerned with the compositions that the structure is similar with Combretastatin A4 and using for depression tubulin polymerization or anti-tumor drug.

In accordance with the present invention, there have been identified extracts from a tropical plant that initiate paclitaxel-like microtubule bundling. Bioassay-directed purification yields the steroid taccalonolide A. Taccalonolide, like paclitaxel, initiates the formation of abnormal interphaes and mitotic microtubules. Cells treated with taccalonolide exhibit thick bundles of microtubules that appear to nucleate independent of the microtubule organizing center. Abnormal mitotic spindles consisting of multi-polar spindles are initiated by taccalonolide and resemble abnormal mitotic spindles found in the presence of paclitaxel. Like paclitaxel, taccalonolide causes the breakdown of the nucleus into micronuclei. Taccalonolide causes G2/M arrest, Bc1-2 phosphorylation and initiates an apoptotic cascade that includes the activation of caspase 3. Taccalonolide is an effective inhibitor of proliferation against both SK-OV-3 and MDA-MB-435 cell with IC₅₀ values of 2.3 μM and 2.1 μM respectively. In contrast to paclitaxel, taccalonolide is effective against the multidrug resistant SKVLB-1 cellline and thus appears to be a poor substrate for P-glycoprotein-mediated transport. Although taccalonolide is almost equipotent with paclitaxel in its effects on cellular microtubules, it is much less potent than paclitaxel in its ability to initiate the polymerization of purified tubulin and microtubule protein. Taccalonolide A is the first microtubule stabilizing agent to be discovered from a plant since identification of the mechanism of action of paclitaxel and it is the first natural product steroid identified to have these cellular effects.

The invention relates to a class of cinnamoyl sulfonamide derivatives, wherein the derivatives are characterized in that the derivatives have the following general formula, and R1 in the structural formula is represented in the picture. The cinnamic acid derivatives of the present invention have effects of tubulin polymerization resistance and mice melanoma cell B16-F10 proliferation inhibition, such that the cinnamic acid derivatives of the present invention can be adopted as potential anti-tumor drugs. The present invention further discloses a production method for the derivatives.