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Org Lett. 2008 Sep 18;10(18):4021-4. doi: 10.1021/ol801532s. Epub 2008 Aug 16.

Synthesis and activity of largazole analogues with linker and macrocycle modification.

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  • 1Department of Chemistry, Duke University, Durham, North Carolina 27708, USA.


To characterize largazole's structural requirements for histone deacetylase (HDAC) inhibitory and antiproliferative activities, a series of analogues with modifications to the side chain or 16-membered macrocycle were prepared and biologically evaluated. Structure-activity relationships suggested that the four-atom linker between the macrocycle and octanoyl group in the side chain and the (S)-configuration at the C17 position are critical to repression of HDAC activity. However, the valine residue in the macrocycle can be replaced with alanine without significant loss of activity.

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