Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.

Basic Information

ID: ALA1157124

Journal: Bioorg Med Chem Lett

Title: Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.

Authors: Zhang SJ, Ge QF, Guo DW, Hu WX, Liu HZ.

Abstract: alpha-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 microg/mL. Compound 17 m was further selected for in vivo evaluation against S180 xenograft in ICR mice, which had 24.7% tumor-weight inhibition through intragastric administration of 200mg/kg of body weight. Moreover, the LD(50) in mice for 17 m through ig exceeded 1000 mg/kg of body weight.

CiteXplore: 20403695

DOI: 10.1016/j.bmcl.2010.03.112

Patent ID: