1,3-Benzodioxole Derivatives Improve the Anti-Tumor Efficiency of Arsenicals.

ABSTRACT: Arsenicals have been widely used in the treatment of cancers such as leukemia and other tumors. However, their side effects limit their clinical application. Stiripentol, a second-line adjunctive treatment for epilepsy with a good safety profile, inhibits microsomal cytochrome-P450-family enzymes to extend the retention time of co-administration. Inspired by the metabolism of stiripentol, the 1,3-benzodioxole responsible for the inhibition and its metabolic derivatives were conjugated with arsenical precursors. The fabricated arsenicals were eliminated much slower in mice and maintained an efficient concentration in the blood for a longer time than that of the arsenical precursors. They also performed better in anti-proliferation by inhibiting the thioredoxin system to induce oxidative str

SUBMITTER: Shi XM 

PROVIDER: S-EPMC9266561 | biostudies-literature | 2022 Jun

REPOSITORIES: biostudies-literature