Anticancer agents based on regulation of protein prenylation

Details Anticancer agents based on regulation of protein prenylation Anticancer agents based on regulation of protein prenylation

C - Chemistry, Metallurgy

12

N

C12N 9/99 (2006.01) A61K 31/00 (2006.01) A61K 31/20 (2006.01) C07C 29/10 (2006.01) C07C 69/63 (2006.01) C07C 217/46 (2006.01) C07C 219/20 (2006.01) C07D 303/32 (2006.01) C07D 303/42 (2006.01)

Patent

CA 2426203

Oncoproteins such as Ras and RhoB are known to induce cell division in an unrestrained manner when such proteins are localized at the inner surface of a cancer cell membrane. The localization is effected by the prenylation reaction, whereby a hydrophobic group (e.g. farnesyl protein transferase). Deactivation of the prenylation enzyme through covalent modification can therefore ultimately result in the mitigation and/or cessation of cancer cell growth. Various prenylation inhibitors having the necessary structural groups to bond covalently, or essentially irreversibly, to the prenylation enzyme include carbonyl or thiocarbonyl compounds (or masked versions of these compounds) and alpha oxo-epoxides bonded to a hydrophobic, substrate-mimicking group. The carbonyl or thiocarbonyl compounds also contain a nucleofugal atom or group to enhance the tendency to form covalent bonds.

L'invention porte sur les oncoprotéines telles que la Ras et RhoB qui ont la particularité d'induire facilement la division cellulaire lorsque ces protéines se trouvent sur la surface interne de la membrane d'une cellule cancéreuse. Leur localisation résulte de la réaction de prénylation au cours de laquelle un groupe hydrophobe (par exemple un groupe farnesyl) se fixe à la protéine en présence d'une enzyme (par exemple la farnesyl protéine transférase). L'inactivation de l'enzyme de prénylation, par modification covalente peut, par conséquent, enfin limiter et/ou stopper le développement des cellules cancéreuses. L'invention porte également sur plusieurs agents inhibiteurs de prénylation possédant les groupes structuraux nécessaires pour se lier par covalence, ou presque définitivement, à l'enzyme de prénylation et contenant des composés carbonyle et thiocarbonyle (ou des versions masquées de ces composées) et des oxo-époxydes alpha liés à un groupe hydrophobe imitant un substrat. Les composés carbonyle et thiocarbonyle contiennent également un atome ou un groupe nucléofuge qui a la propriété de favoriser la formation de liaisons covalentes.

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