Analogs of green tea polyphenols as chemotherapeutic and...

Details Analogs of green tea polyphenols as chemotherapeutic and... Analogs of green tea polyphenols as chemotherapeutic and...

C - Chemistry, Metallurgy

07

D

C07D 311/62 (2006.01) A61K 31/353 (2006.01) A61P 35/00 (2006.01)

Patent

CA 2508020

Novel compounds useful as chemotherapeutic and chemopreventive agents are provided. The compounds are analogs of polyphenol catechins that occur in green tea, such as epigallocatichin-3-gallate (EGCG), and have the structure of formula (I) wherein R1through R11 are defined herein. Preferred R4 moieties are selected from 0, S, NH and CH2, and in exemplary compounds, R4 is 0 and R5 is a tri-substituted aroyloxy substituent, such as a 3,4,5-substituted benzoyloxy group. Pharmaceutical compositions are provided as well, as are methods of chemotherapy and chemoprevention.

La présente invention a trait à de nouveaux composés utiles en tant qu'agents chimiothérapeutiques et chimiopréventifs. Les composés sont des analogues de catéchines de polyphénol présents dans le thé vert, telles que l'épigallocathichine-3-gallate (EGCG), et présentent la structure de formule (I), dans laquelle: R?1¿ à R?11¿ sont tels que définis dans la description. Les groupes fonctionnels R?4¿ préférés sont sélectionnés parmi O, S, NH et CH¿2?, et dans des composés représentatifs, R?4¿ est O et R?5¿ est un substituant aryloxy trisubstitué, tels qu'un groupe benzoyloxy substitué en position 3, 4 et 5. L'invention a également trait à des compositions pharmaceutiques, ainsi que des procédés de chimiothérapie et de chimioprévention.

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