Novel Flavaglines Displaying Improved Cytotoxicity

作者:Thuaud Frederic; Ribeiro Nigel; Gaiddon Christian; Cresteil Thierry; Desaubry Laurent*
来源:Journal of Medicinal Chemistry, 2011, 54(1): 411-415.
DOI:10.1021/jm101318b

摘要

Novel flavagline analogues were synthesized and examined with respect to their cytotoxicity Structural features critical to the potential of this class of anticancer natural products wet e unraveled We demonstrated, in particular, that the introduction of substituants at C-2 has a deleterious effect on multidrug resistance Replacement of the hydroxy at C-1 by an aminoformyl with the opposite configuration enhances the cytotoxicity and led to a compound that reduces tumors growth in an allograft model at nontoxic doses

  • 出版日期2011-1-13