Synthetic spiroketal pyranes as potent anti-cancer agents

Details Synthetic spiroketal pyranes as potent anti-cancer agents Synthetic spiroketal pyranes as potent anti-cancer agents

C - Chemistry, Metallurgy

07

K

C07K 14/47 (2006.01) A61K 31/35 (2006.01) C07D 311/00 (2006.01) C07D 493/10 (2006.01)

Patent

CA 2336294

Novel tubulin binding compounds (SPIKETS) 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 SP binding pocket on tubulin, which pocket is useful for screening of anti-tubulin, anti-proliferation, and anti-cancer drugs.

L'invention concerne des composés nouveaux (portant l'appellation SPIKET en anglais), 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 spongistatine sur la tubuline, ladite poche étant utile pour le dosage des médicaments antitubuline, antiprolifération et anticancéreux.

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