Inventors:
Ralph A. Zingaro - College Station TX, US
Emil J. Freireich - Houston TX, US
Hatice Duzkale - Houston TX, US
Hagop Kantarjian - Bellaire TX, US
Srdan Verstovsek - Houston TX, US
Merida Sotelo-Lerma - Hermosillo, MX
Assignee:
The Texas A&M University System - College Station TX
Board of Regents, The University of Texas System - Austin TX
International Classification:
A61K 31/285, A61K 33/36, C07F 9/00
US Classification:
514504, 556 71, 556 77, 556 78, 556 80, 424629
Abstract:
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-glutathione, S-dimethylarsino-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-thiobenzoic acid, and other organic arsenicals as an anti-cancer therapy, combining high efficacy with very low, if any, toxicity.