Anti-mitotic agents which inhibit tubulin polymerization

Details Anti-mitotic agents which inhibit tubulin polymerization Anti-mitotic agents which inhibit tubulin polymerization

C - Chemistry, Metallurgy

07

D

C07D 333/64 (2006.01) C07C 43/205 (2006.01) C07C 43/23 (2006.01) C07C 49/115 (2006.01) C07C 49/84 (2006.01) C07C 205/37 (2006.01) C07D 307/80 (2006.01) C07D 333/56 (2006.01)

Patent

CA 2283471

Methoxy and ethoxy substituted 3-aroyl-2-arylbenzo[b]thiophenes and benzo[b]thiophene analogues are described for use in inhibiting tubulin polymerization. The compounds' use for treating tumor cells is also described. Additional aspects described here are certain diaryl ether benzo[b]thiophene derivatives. Also described are particular analogs derived from dihydronaphthalene which have proven particularly effective. Certain new benzofuran analogs are described, as well as certain sulfur oxide benzo[b]thiophene analogs. Important compounds described herein include the first nitrogen-containing derivatives of combretastatin. These include nitro, amino and azide combretastatin derivatives.

L'invention concerne des 3-aroyl-2-arylbenzo[b]thiophènes méthoxy et éthoxy substitués, et des analogues de benzo[b] thiophène, s'utilisant pour inhiber la polymérisation de tubuline. L'invention concerne également l'utilisation du composé dans le traitement de cellules tumorales. L'invention concerne dans d'autres certains dérivés d'éther de diaryle benzo[b] thiophène, ainsi que des analogues particuliers dérivés de dihydronaphthalène qui se sont révélés particulièrement efficaces. L'invention concerne également de nouveaux analogues de benzofuranne, ainsi que des analogues d'oxyde de soufre benzo[b]thiophène. Des composés importants selon l'invention comprennent les premiers dérivés de combrétastatine contenant du nitrogène, y compris des dérivés de combrétastatine nitrés, aminés, et d'azide.

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