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.