38 results about "Tubulin Polymerization Inhibitors" patented technology

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 isoquinolines and their use as tubulin polymerization inhibitors. In particular, the invention relates to substituted isoquinolines which possess useful therapeutic activity, use of these compounds in methods of therapy and the manufacture of medicaments as well as compositions containing these compounds.

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 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 (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 relates to the field of medicine and specifically relates to application of a microtubule polymerization inhibitor (which is shown in a formula I) containing a pyrazoline structure in preparing drugs for treating and resisting tumor.

The invention discloses a synthesis method of Combretastatin A-4 derivatives. Aiming at double targets of BFGF and tubulin, a tubulin polymerization inhibitor CA-4 and its analogues are respectively coupled with aminosugar having BFGF inhibition effects so that eight novel compounds are designed and synthesized. A preliminary pharmacological test result shows that the desired compounds have human umbilical vein endothelial cell proliferation inhibition effects superior to that of a positive drug CA-4.

An aspect described herein includes a method for treating acute myeloid leukemia (AML) in a subject in need thereof comprising, administering to the subject an effective amount of a small molecule tubulin polymerization inhibitor compound. More particularly, another aspect described herein includes a method for treating acute myeloid leukemia in a subject in need thereof comprising, administering to the subject an effective amount of the small molecule tubulin polymerization inhibitor compound described herein in combination with a chemotherapeutic agent.