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.
Publication types
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Research Support, N.I.H., Extramural
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Research Support, Non-U.S. Gov't
MeSH terms
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Depsipeptides / chemical synthesis*
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Depsipeptides / chemistry
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Depsipeptides / pharmacology*
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Histone Deacetylase Inhibitors*
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Marine Biology
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Models, Molecular
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Molecular Structure
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Structure-Activity Relationship
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Thiazoles / chemical synthesis*
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Thiazoles / chemistry
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Thiazoles / pharmacology*
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Zinc / chemistry*
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Zinc / pharmacology
Substances
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Depsipeptides
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Histone Deacetylase Inhibitors
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Thiazoles
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largazole
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Zinc