C - Chemistry – Metallurgy – 07 – F
Patent
C - Chemistry, Metallurgy
07
F
C07F 9/74 (2006.01) A61K 31/285 (2006.01) A61P 35/00 (2006.01) C07F 9/72 (2006.01)
Patent
CA 2472633
Arsenic trioxide, an inorganic compound, is commercially available anti-cancer agent but it carries significant toxicity. Organic arsenicals, on the other hand, are much less toxic, to the extent that the methylation of inorganic arsenic in vivo into organic arsenicals has been considered a detoxification reaction. New organic arsenic derivatives have been synthesized, including S- dimethylarsino-glutatione, S-dimethylarisno-thiosuccinic acid and S- dimethylarsino-thiobenzoic acid, and established its potent in vitro cytotoxic activity against numerous human tumor cell lines, both of solid and hematological origin, as well as against malignant blood cells from patients with leukemia. Results form a basis for the development of S-dimethylarsino- glutathione, S-dimethylarsino-thiosuccinic acid, S-dimethylarsino-thiobenzonic acid, and other organic arsenicals as an anti-cancer therapy, combining high efficacy with very low, if any, toxicity.
Le trioxyde d'arsenic, un composé inorganique, est un agent anticancéreux commercialement disponible, mais présentant une toxicité importante. Les composés arsenicaux organiques sont en revanche beaucoup moins toxiques, au point que la méthylation de l'arsenic inorganique in vivo en arsenicaux organiques a été considérée comme une réaction de détoxication. Cette invention concerne des dérivés d'arsenic nouvellement synthétisés, à savoir le S-diméthyl-arsino-glutatione, l'acide S-diméthyl-arsino-thiosuccinique et l'acide S-diméthyl-arsino-thiobenzoïque, dont l'activité in vitro contre un grand nombre de lignées de cellules tumorales humaines, d'origine solide ou hématologique, ainsi que contre les cellules sanguines malignes provenant de patients leucémiques a été démontrée. Ces résultats constituent la base pour la mise au point de S-diméthyl-arsino-glutathione, d'acide S-diméthyl-arsino-thiosuccinique, d'acide S-diméthyl-arsino-thiobenzonique, et d'autres arsenicaux organiques utilisables comme traitement anticancéreux, qui présentent une efficacité élevée combinée à une toxicité très faible, voire nulle.
Duzkale Hatice
Freireich Emil L.
Kantarjian Hagop
Sotelo-Lerma Merida
Verstovsek Srdan
Board Of Regents The University Of Texas System
Goudreau Gage Dubuc
The Texas A. & M. University System
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