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Synfacts 2008(7): 0669-0669  
DOI: 10.1055/s-2008-1077866
Synthesis of Natural Products and Potential Drugs
© Georg Thieme Verlag Stuttgart · New York

Synthesis of FK228

Contributor(s): Philip Kocienski, Indu Dager
T. J. Greshock, D. M. Johns, Y. Noguchi, R. M. Williams*
Colorado State University, Fort Collins and The University of Colorado Cancer CentER, Aurora, USA
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Publication History

Publication Date:
20 June 2008 (online)

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Significance

Isolated from the fermentation broth of Chromobacterium violaceum, the cyclo­depsi-peptide FK228 is a potent HDAC inhibitor. It inhibits murine and human solid tumor cells; it also targets the epigenetic silencing mechanism crucial to carcinogenesis. A convergent scaleable synthesis of FK228 is reported here, where both the fragments C and F were prepared on multigram scale starting from commercially available materials.