Syntheses of amamistatin fragments and determination of their HDAC and antitumor activity.

Kelley A Fennell, Marvin J Miller

Department of Chemistry and Biochemistry, University of Notre Dame, Notre Dame, Indiana 46556, USA.

Organic letters 2007 Apr 26

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reaction: see text] Amamistatins A and B are natural products found to have anti-proliferative effects against MCF-7, A549, and MKN45 human tumor cell lines (IC50 0.24-0.56 microM). It was proposed that their activity was due to histone deacetylase (HDAC) inhibition mediated by the N-formyl-N-hydroxy lysine moiety. Amamistatin B fragment analogs were synthesized and screened for biological activity. These compounds were modest HDAC inhibitors and showed antitumor activity against MCF-7 and PC-3 human tumor cells.

Citation

Kelley A Fennell, Marvin J Miller. Syntheses of amamistatin fragments and determination of their HDAC and antitumor activity. Organic letters. 2007 Apr 26;9(9):1683-5