Synthesis and anticancer evaluation of α-lipoic acid derivatives

SJ Zhang, QF Ge, DW Guo, WX Hu, HZ Liu

Index: Zhang, Shi-Jie; Ge, Qiu-Fu; Guo, Dian-Wu; Hu, Wei-Xiao; Liu, Hua-Zhang Bioorganic and Medicinal Chemistry Letters, 2010 , vol. 20, # 10 p. 3078 - 3083

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Citation Number: 17

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 100μg/mL. Compound 17m was further selected for in vivo evaluation against S180 xenograft in ICR mice, which had 24.7% tumor-weight inhibition ...