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Article Dans Une Revue Bioorganic and Medicinal Chemistry Année : 2008

Synthesis and cytotoxic activities of usnic acid derivatives.

Résumé

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.

Dates et versions

hal-00298610 , version 1 (16-07-2008)

Identifiants

Citer

Marc-Antoine Bazin, Anne-Cécile Le Lamer, Jean-Guy Delcros, Isabelle Rouaud, Philippe Uriac, et al.. Synthesis and cytotoxic activities of usnic acid derivatives.. Bioorganic and Medicinal Chemistry, 2008, 16 (14), pp.6860-6866. ⟨10.1016/j.bmc.2008.05.069⟩. ⟨hal-00298610⟩
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