38 results about "Tubulin Polymerization Inhibitors" patented technology

The present invention relates to compounds of general formula (I) as tublin polymerisation inhibitors and methods for preparing such compounds.

A pharmaceutical composition of a tubulin polymerisation inhibitor and an mTOR inhibitor and a method of treating proliferative disease with a combination of a tubulin polymerisation inhibitor and an mTOR inhibitor.

A novel series of BPU analogues were synthesized and evaluated for antitumor activity. In particular, BPU sulfur analogues 6n and 7d were shown to possess up to 10-fold increased potency, when compared to compound 1, against cancer cell lines. 6n was more effective than compound 1 in causing apoptosis of MCF-7 cells. When compared to other drugs with a similar mechanism of action, 6n retained significant ability to inhibit tubulin assembly, with an IC50 of 2.1 μM.

The present invention relates generally to substituted benzofurans, benzothiophenes, and indoles and their use as tubulin polymerization inhibitors.

The present invention relates to application of IMB5046 compound in the preparation of antineoplastic drugs. The antineoplastic drug is composed of, by weight, 0.1-99.9% of a compounds shown as a formula I and 0.1-99.9% of pharmaceutically acceptable excipients. The compound shown as formula I can inhibit the polymerization of tubulin and destroy microtubules within cells, has strong cytotoxic activity on tumor cells, especially drug-resistant cells, and can inhibit the growth of xenograft tumor in nude mice. The compound is a tubulin polymerization inhibitor with a novel structure, and has good prospects in developing into antineoplastic drug.

The present invention relates to compounds of general formula (I) as tublin polymerization inhibitors and methods for preparing such compounds.

The invention discloses a class of sulfonamide-1,2,3-triazole-containing compounds, their preparation method and their application in Tubulin polymerization inhibitors, belonging to the field of antitumor pharmaceutical chemistry. The present invention uses classic click chemistry to combine the sulfa-1,2,3-triazole active unit with the sulfa-1,2,3-triazole active unit, thereby synthesizing the sulfa-1,2,3-triazole compounds in a simple, efficient, and environmentally friendly manner. It has the following general structural formula: the in vitro anticancer activity test of this type of compound shows that it has a certain inhibitory effect on a variety of tumor cells PC-3, MCF-7, MGC-803, and has a significant inhibitory effect on the polymerization of Tubuli , which can be used as a candidate or lead compound for further development in the preparation of antitumor drugs.

The invention discloses a pyridine-2-aryl-3-sulfonamide compound, its synthesis method and its application in the preparation of antitumor drugs or tubulin polymerization inhibitors. The pyridine-2-aryl-3-sulfonamide compound of the present invention has the general structural formula (I), X, Y, Z are taken from C or N atom, R 1 Represents a monosubstituted or polysubstituted group; R 2 Represents a monosubstituted or polysubstituted group; R 3 Represents hydrogen or benzenesulfonyl substituted by different C1-5 alkoxy groups. The application of pyridine-2-aryl-3-sulfonamide compounds in the preparation of medicines is used as an active ingredient for the preparation of antitumor medicines or tubulin polymerization inhibitors. The antitumor drugs are anti-colon cancer, anti-breast cancer, anti-liver cancer, anti-lung cancer, anti-gastric cancer or anti-pancreatic cancer drugs.

The invention discloses novel three-stage amide microtubulin polymerization inhibitors, a preparation method of the novel three-stage amide microtubulin polymerization inhibitors and application thereof to medicine for treating gastric cancer, prostatic cancer, breast cancer and the like, and belongs to the field of anti-tumor medicine chemistry. A kind of novel microtubulin polymerization inhibitors are synthesized in an efficient green and environment-friendly way. The inhibitors have the following structure general formula shown in the description. The in vitro anticancer activity experiments prove that the inhibitors have certain inhibition effects on various tumor cells PC3, MCF7 and MGC803; meanwhile, the obvious inhibition effects are achieved on microtubulin. The activity of compounds (IId, IIe, IIg, IIi, IIm, IIo, IIp, IIq and IIr) on three kinds of cancer cells is better than that of anti-tumor medicine 5-fluorouracil. The inhibitors can be applied to anti-tumor medicine preparation through being used as candidate or lead compounds for further development.

The invention relates to the field of medicine, in particular to the use of a novel tubulin polymerization inhibitor (general formula I) containing a pyrazoline structure in the preparation of antitumor drugs.

The present invention relates to (E)-ethyl 2-(2-methyl-3-((2-(naphtho[2,1-b]furan-2-carbonyl)hydrazono)methyl)-1H-indol-1-yl)acetate as a novel tubulin polymerization inhibitor and a method for synthesizing the same. The compound of the present invention can inhibit mitosis and induce apoptosis and thus be used as an anticancer agent, by binding to tubulin to inhibit microtube polymerization. According to the synthesis method of the present invention, the reaction is simplified and the efficiency is 60% or higher, leading to a very high yield, thereby providing an effective synthesis method.

Substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carbonitriles and substituted 4-amino-5-benzoyl-2-(phenylamino)thiophene-3-carboxamides and their salts are tubulin polymerization inhibitors, useful in the treatment of cancer.

Methods and combination therapies for treating, preventing, and / or delaying the onset and / or development of cancer using a tubulin polymerization inhibitor such as a compound of formula I, or a pharmaceutically acceptable salt thereof, and a poly (ADP-ribose) polymerase (PARP) inhibitor,or a pharmaceutically acceptable salt thereof, are provided.

The invention is directed to compounds having the following structures:N-(3-ethoxyphenyl)-1,4-dihydro-6-ethoxy-7-(3-hydroxypropoxy)-1-methylindeno[1,2-c]pyrazole-3-amine;3-[3-(3-Bromo-phenylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol;or3-[3-(2-Chloro-pyridin-4-ylamino)-6-ethoxy-1-methyl-1,4-dihydro-indeno[1,2-c]pyrazol-7-yloxy]-propan-1-ol, and N-oxides, pharmaceutically acceptable salts, solvates, tautomers and stereochemical isomers thereof and the uses of such compounds as inhibitors of tubulin polymerization and for the treatment of solid tumors. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.