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Novel flavaglines displaying improved cytotoxicity.

Abstract：

: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 were 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.

journal_name

J Med Chem

journal_title

Journal of medicinal chemistry

authors

Thuaud F,Ribeiro N,Gaiddon C,Cresteil T,Désaubry L

doi

10.1021/jm101318b

subject

Has Abstract

pub_date

2011-01-13 00:00:00

pages

411-5

issue

1

eissn

0022-2623

issn

1520-4804

journal_volume

54

pub_type

杂志文章

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