Epothilone analogs

Details Epothilone analogs Epothilone analogs

C - Chemistry, Metallurgy

07

D

C07D 493/04 (2006.01) C07D 313/00 (2006.01) C07D 405/06 (2006.01) C07D 407/06 (2006.01) C07D 409/06 (2006.01) C07D 413/06 (2006.01) C07D 417/06 (2006.01)

Patent

CA 2274833

Epothilone A, epothilone B, analogs of epothilone and libraries of epothilone analogs are synthesized. Epothilone A and B are known anticancers agents that derive their anticancer activity by the prevention of mitosis through the induction and stabilization of microtubulin assembly. The analogs of epothilone are novel. Several of the analogs are demonstrated to have a superior cytotoxic activity as compared to epothilone A or epothilone B as demonstrated by their enhanced ability to induce the polymerization and stabilization of microtubules.

L'invention concerne épothilone A, épothilone B, des analogues d'épothilone et des bibliothèques d'épothilone synthétisés. Les épothilones A et B sont connus comme agents anticancéreux dont l'activité anticancéreuse est due à la prévention de la mitose par induction et stabilisation de l'assemblage de la microtubuline. Les analogues d'épothilone sont nouveaux. Il est démontré que plusieurs des analogues ont une activité cytotoxique supérieure comparé à épothilone A ou épothilone B, comme l'atteste leur capacité accrue d'induction de la polymérisation et de la stabilisation des microtubules.

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