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Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold.
|Publication Type||Journal Article|
|Authors||Bowers, AA, West N., Newkirk TL, Troutman-Youngman AE, Schreiber SL, Wiest O., Bradner JE, and Williams RM|
|Abstract||Fourteen 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 Publication||2009|
|Date Published (YYYY/MM/DD)||2009/03/19|