Human cancer inhibitory pentapeptide heterocyclic and...

C - Chemistry – Metallurgy – 07 – K

Patent

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C07K 7/02 (2006.01) C07K 1/06 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2203689

The synthesis and elucidation of nineteen heterocyclic or halophenyl amide derivatives of dolastatin (10) are disclosed. These compounds and the methods of producing those compounds offer demonstrated significant in vitro activity against several human cancer cell lines. These compounds and the methods of producing those compounds offer a commercially viable alternative to natural and synthetic dolastatin (10).

Cette invention concerne la synthèse et l'élucidation de dix-neuf dérivés amide hétérocyclique ou halophénylique de dolastatine 10. Il a été démontré que ces composés, considérés avec leur procédés de fabrication, ont une activité in vitro importante dans la lutte contre plusieurs lignées cellulaires cancéreuses chez l'homme. Ces composés, ainsi que leurs procédés de fabrication, offrent une alternative viable, d'un point de vue commercial, à la dolastatine 10, qu'elle soit naturelle ou synthétique.

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