Tubulin binding compounds (cobra)

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

C07D 307/12 (2006.01) A61K 31/16 (2006.01) A61K 31/34 (2006.01) C07C 323/41 (2006.01) C07D 307/42 (2006.01) C07K 14/47 (2006.01)

Patent

CA 2336309

Novel tubulin binding compounds having potent tubulin depolymerization activity and inhibitory activity against tubulin polymerization. The compounds are effective agents for inhibiting cellular proliferation, for example, in cancer cells. The compounds are adapted to interact favorably with a novel tubulin binding pocket, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

L'invention concerne des composés nouveaux, capables de se lier avec la tubuline et ayant de ce fait une puissante action de dépolymérisation de la tubuline et un puissant effet inhibiteur sur la polymérisation de la tubuline. Lesdits composés sont efficaces comme inhibiteurs de la prolifération cellulaire, par exemple dans les cellules cancéreuses. Ils peuvent entrer en interaction favorable avec une nouvelle poche de liaison de la tubuline, ladite poche étant utile pour le dosage des médicaments antitubuline, antiprolifération et anticancéreux.

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