Spiro derivatives of parthenin as novel anticancer agents

Details Spiro derivatives of parthenin as novel anticancer agents Spiro derivatives of parthenin as novel anticancer agents

C - Chemistry, Metallurgy

07

D

C07D 498/10 (2006.01) A61K 31/396 (2006.01) A61K 31/4192 (2006.01) A61K 31/424 (2006.01) A61P 35/00 (2006.01) C07D 491/107 (2006.01)

Patent

CA 2728855

The present invention relates to novel spiro derivatives of parthenin prepared by the dipola cycloaddition of various dipoles viz, benzonitrile oxides, nitrones, azides, nitrile ylide diazoalkane, nirile imide, ozone, azomethine imides, azomethine ylides etc. with exocycli double bond of C ring (.alpha.-methylene-.gamma.- butyrolactone). Representative compounds have bee screened for their anticancer activity against different cancer cell lines. IC s0 value of thes analogues varies between 4.3 µM to 93 µM. A mechanistic correlation of their anticance activity has been described. The results of the cytotoxicity test of the compounds studie indicated that the .alpha., .beta.-unsaturated ketonic moity in parthenin plays an important role in th maintenance of the high level of cytotoxicity.

La présente invention concerne de nouveaux dérivés spiro de parthénine préparés par la cycloaddition dipolaire de divers dipôles comme, par exemple, d'oxydes de benzonitrile, de nitrones, d'azides, de diazoalkane d'ylure de nitrile, de nitrile imide, d'ozone, d'imides d'azométhine, d'ylures d'azométhine, etc., avec une double liaison exocyclique d'anneau C (a-méthylène-?-butyrolactone). Des composés représentatifs ont été comparés, en termes de leur activité anticancéreuse, à différentes lignes cellulaires cancéreuses. La valeur ICs0 de ces analogues varie entre 4,3 µM et 93 µM. Une corrélation mécanistique de leur activité anticancéreuse a été décrite. Les résultats du test de cytotoxicité de l'étude des composés ont fait apparaître que le fragment cétonique a, ß-insaturé dans la parthénine joue un rôle important dans le maintien du niveau élevé de cytotoxicité.

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