title: Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
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.
authors.affiliation: College of Pharmaceutical Science, Zhejiang University of Technology, Hangzhou 310032, PR China.
authors.forename: Shi-Jie
authors.initials: SJ
authors.lastname: Zhang
authors.forename: Qiu-Fu
authors.initials: QF
authors.lastname: Ge
authors.forename: Dian-Wu
authors.initials: DW
authors.lastname: Guo
authors.forename: Wei-Xiao
authors.initials: WX
authors.lastname: Hu
authors.forename: Hua-Zhang
authors.initials: HZ
authors.lastname: Liu
mesh_terms: D000818:Animals; D000970:Antineoplastic Agents / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology; D045744:Cell Line, Tumor; D004353:Drug Evaluation, Preclinical; D004354:Drug Screening Assays, Antitumor; D006801:Humans; D051379:Mice; D013329:Structure-Activity Relationship; D008063:Thioctic Acid / Q000031:analogs & derivatives* / Q000138:chemical synthesis / Q000737:chemistry* / Q000494:pharmacology; D023041:Xenograft Model Antitumor Assays
chemical_list: D000970:Antineoplastic Agents; D008063:Thioctic Acid