New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation

Baud, Matthias, Leiser, Thomas, Meyer-Almes, Franz-Josef and Fuchter, Matthew J. (2011) New synthetic strategies towards psammaplin A, access to natural product analogues for biological evaluation. Organic & Biomolecular Chemistry, 9 (3), 659-662. (doi:10.1039/C0OB00824A).

Record type: Article

Abstract

New synthetic routes towards the natural product psammaplin A were developed with the particular view to preparing diverse analogues for biological assessment. These routes utilize cheap and commercially available starting materials, and allowed access to psammaplin A analogues not accessible via currently reported methods. Preliminary biological studies revealed these compounds to be the most potent non peptidic inhibitors of the enzyme histone deacetylase 1 (HDAC1, class I) discovered so far. Interestingly, psammaplin A and our synthetic analogues show class I selectivity in vitro, an important feature for the design and synthesis of future isoform selective inhibitors.

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