Preliminary studies of new proteasome inhibitors in the tumor targeting approach: synthesis and in vitro cytotoxicity

…, P Auzeloux, J Sauzieres, JC Madelmont

文献索引：Vivier, Magali; Jarrousse, Anne-Sophie; Bouchon, Bernadette; Galmier, Marie-Josephe; Auzeloux, Philippe; Sauzieres, Jacques; Madelmont, Jean-Claude Journal of Medicinal Chemistry, 2005 , vol. 48, # 21 p. 6731 - 6740

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被引用次数: 19

摘要

The proteasome is a multicatalytic protease that plays a critical role in the cell. The control of proteasomes could, thus, provide a weapon for the treatment of cancer. Therefore, we have synthesized six new peptide aldehyde inhibitors of the proteasome linked to the N-(2- diethylaminoethyl) benzamide (BZA-CO) structure, in order to target the cytotoxic activity to malignant melanoma cells. Biological studies demonstrated the influence of length and ...