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Synthesis and anticancer evaluation of alpha-lipoic acid derivatives.
- Source :
-
Bioorganic & medicinal chemistry letters [Bioorg Med Chem Lett] 2010 May 15; Vol. 20 (10), pp. 3078-83. Date of Electronic Publication: 2010 Apr 03. - Publication Year :
- 2010
-
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.<br /> (Copyright 2010 Elsevier Ltd. All rights reserved.)
- Subjects :
- Animals
Antineoplastic Agents chemistry
Antineoplastic Agents pharmacology
Cell Line, Tumor
Drug Evaluation, Preclinical
Drug Screening Assays, Antitumor
Humans
Mice
Structure-Activity Relationship
Thioctic Acid chemical synthesis
Thioctic Acid pharmacology
Xenograft Model Antitumor Assays
Antineoplastic Agents chemical synthesis
Thioctic Acid analogs & derivatives
Thioctic Acid chemistry
Subjects
Details
- Language :
- English
- ISSN :
- 1464-3405
- Volume :
- 20
- Issue :
- 10
- Database :
- MEDLINE
- Journal :
- Bioorganic & medicinal chemistry letters
- Publication Type :
- Academic Journal
- Accession number :
- 20403695
- Full Text :
- https://doi.org/10.1016/j.bmcl.2010.03.112