Jean M. Brunel, Chanaz Salmi-Smail, Audrey Restouin, Thomas Prebet, Norbert Vey and Yves Collette Pages 801 - 806 ( 6 )
A series of N-substituted amino caproic hydroxamic acid histone deacetylase inhibitors derivatives was designed in good-toexcellent yields and evaluated for their antiproliferative activity in a panel of human cancer cell lines, showing half maximum effective concentration varying from 700 nM to > 100 μM. Interestingly, the replacement of a furyl group by a thienyl one impacted very significantly the cap role on this antiproliferative activity and on histone acetylation induced by these drugs in cell-based but also in cell-free enzyme assays, suggesting an important role of the electronic density attached to the oxygen or sulfur atoms.
N-substituted amino caproic hydroxamic acid, Histone deacetylase inhibitors, Anticancer agents, SAHA derivatives, carcinogenesis, dichloromethane, chromatography, aminohexanoic.
Aix-Marseille Universite, Centre de Recherche en Cancerologie de Marseille (CRCM), Laboratory of Integrative Structural & Chemical Biology (iSCB), UMR CNRS 7258, Inserm-U1068, Faculte de Pharmacie, 27 Bd Jean Moulin, 13385 Marseille Cedex 05, France.