Synthesis and anticancer evaluation of α-lipoic acid derivatives

Abstract α-Lipoic acid derivatives were synthesized and evaluated for their in vitro anticancer activities against NCI-460, HO-8910, KB, BEL-7402, and PC-3 cell lines. The results, for most compounds exhibited dose-dependent inhibitory property and several compounds had good inhibitions at the dose of 100 μg/mL. Compound 17m was further selected for in vivo evaluation against S180 xenograft in ICR mice, which had 24.7% tumor-weight inhibition through intragastric administration of 200 mg/kg of body weight. Moreover, the LD 50 in mice for 17m through ig exceeded 1000 mg/kg of body weight.