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 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 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 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.

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.