Polythiophene anti-tumor agents

A - Human Necessities – 61 – K

Patent

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Details

A61K 31/38 (2006.01) A61K 31/381 (2006.01) C07D 333/14 (2006.01) C07D 333/16 (2006.01) C07D 333/18 (2006.01) C07D 333/22 (2006.01) C07D 333/28 (2006.01) C07D 333/30 (2006.01) C07D 333/32 (2006.01) C07D 333/38 (2006.01)

Patent

CA 2272275

Novel polythiophene compounds useful as anti-tumor agents are described. Preferred compounds of formula (I) wherein n is 0-2 and R2 and R3 are optionally substituted 2-thienyl or 3-thienyl have been found to exhibit selective cytotoxic activity against transformed human cells. Pharmaceutical compositions containing the described polythiophene compounds are expected to exhibit good chemotherapeutic activity against slow growing tumors based on tumor cell line assays. A method for treating patients having tumors utilizing the disclosed polythiophene compounds is also described.

L'invention a trait à des composés à base de polythiofène, efficaces en tant qu'agents antinéoplastiques. Les composés préférés de l'invention répondent à la formule (I) dans laquelle la valeur de n est comprise entre 0 et 2 et dans laquelle R¿2? et R¿3? représentent 2-thiényle ou 3-thiényle éventuellement substitués. Il s'est avéré que ces composés font montre d'une action cytotoxique sélective à l'encontre de cellules humaines transformées. On attend de compositions à usage pharmaceutique contenant les composés à base de polythiofène susmentionnés qu'elles aient une action chimiothérapeutique efficace contre des tumeurs à croissance lente et ce, si l'on se réfère aux criblages effectués sur des lignées cellulaires tumorales. L'invention porte également sur une méthode thérapeutique à l'intention de patients soufrant de tumeurs, méthode faisant intervenir les composés susmentionnés à base de polythiofène.

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