Novel Flavaglines Displaying Improved Cytotoxicity

被引:50
作者
Thuaud, Frederic [1 ]
Ribeiro, Nigel [1 ]
Gaiddon, Christian [2 ]
Cresteil, Thierry [3 ]
Desaubry, Laurent [1 ]
机构
[1] Univ Strasbourg, Dept Med Chem, Fac Pharm, CNRS,Therapeut Innovat Lab UMR 7200, F-67401 Illkirch Graffenstaden, France
[2] Univ Strasbourg, Fac Med, INSERM, Lab Signalisat & Neurodegeneresence UMRS692, F-67085 Strasbourg, France
[3] CNRS, Inst Chim Subst Nat UPR 2301, F-91198 Gif Sur Yvette, France
关键词
ROCAGLAMIDE DERIVATIVES; AGLAIA-ELLIPTICA; LIGNANS; CELLS; APOPTOSIS; GROWTH;
D O I
10.1021/jm101318b
中图分类号
R914 [药物化学];
学科分类号
100701 ;
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
引用
收藏
页码:411 / 415
页数:5
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