1. Synthesis and cytotoxic activities of usnic acid derivatives.
- Author
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Bazin MA, Le Lamer AC, Delcros JG, Rouaud I, Uriac P, Boustie J, Corbel JC, and Tomasi S
- Subjects
- Animals, Antineoplastic Agents chemical synthesis, Apoptosis drug effects, Benzofurans chemical synthesis, CHO Cells, Carrier Proteins, Cell Line, Tumor, Cricetinae, Cricetulus, Humans, Mice, Polyamines, Structure-Activity Relationship, Antineoplastic Agents chemistry, Benzofurans chemistry, Benzofurans pharmacology
- Abstract
Nine usnic acid-amine conjugates were evaluated on murine and human cancer cell lines. The polyamine derivatives showed significant cytotoxicity in L1210 cells. Their activities appeared to be independent of the polyamine transport system (PTS). Indeed, their activities were similar in chinese hamster ovary (CHO) and in the PTS deficient CHO-MG cells. In addition, alpha-difluoromethylornithine, an ornithine decarboxylase inhibitor known to indirectly enhance the activity of the PTS and consequently increase the cytotoxicity of cytotoxic drugs entering cells via the PTS, had no effect on the activity of the polyamine derivatives. The more active derivative (1,8-diaminooctane derivative) displayed similar activities on all cancer cell lines studied and induced apoptosis.
- Published
- 2008
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