Scientific Publications

Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold.

Publication TypeJournal Article
AuthorsBowers, AA, West N., Newkirk TL, Troutman-Youngman AE, Schreiber SL, Wiest O., Bradner JE, and Williams RM
AbstractFourteen analogs of the marine natural product largazole have been prepared and assayed against histone deacetylases (HDACs) 1, 2, 3, and 6. Olefin cross-metathesis was used to efficiently access six variants of the side-chain zinc-binding domain, while adaptation of our previously reported modular synthesis allowed probing of the macrocyclic cap group.
Year of Publication2009
JournalOrganic letters
Date Published (YYYY/MM/DD)2009/03/19
ISSN Number1523-7060