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

…, P Auzeloux, J Sauzieres, JC Madelmont

Index: 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

Full Text: HTML

Citation Number: 19

Abstract

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 ...