Article ID | Journal | Published Year | Pages | File Type |
---|---|---|---|---|
1371731 | Bioorganic & Medicinal Chemistry Letters | 2010 | 6 Pages |
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 LD50 in mice for 17m through ig exceeded 1000 mg/kg of body weight.
Graphical abstractα-Lipoic acid derivatives were synthesized and their anticancer activities were evaluated.Figure optionsDownload full-size imageDownload as PowerPoint slide