Synthesis and histone deacetylase inhibitory activity of largazole analogs: alteration of the zinc-binding domain and macrocyclic scaffold.
Org Lett
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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
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Journal | Org Lett
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Volume | 11
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Issue | 6
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Pages | 1301-4
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Date Published | 2009 Mar 19
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ISSN | 1523-7052
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DOI | 10.1021/ol900078k
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PubMed ID | 19239241
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PubMed Central ID | PMC2673910
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Grant list | CA136283 / CA / NCI NIH HHS / United States
F32 CA136283-01 / CA / NCI NIH HHS / United States
GM49631 / GM / NIGMS NIH HHS / United States
1K08CA128972 / CA / NCI NIH HHS / United States
F32 CA136283 / CA / NCI NIH HHS / United States
R01 GM068011-05A1 / GM / NIGMS NIH HHS / United States
R01 GM068011 / GM / NIGMS NIH HHS / United States
K08 CA128972 / CA / NCI NIH HHS / United States
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