Journal
JOURNAL OF MEDICINAL CHEMISTRY
Volume 54, Issue 21, Pages 7453-7463Publisher
AMER CHEMICAL SOC
DOI: 10.1021/jm200432a
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Funding
- NIH [CA51085]
- Samuel Waxman Cancer Research Foundation
- Susan G. Komen for the Cure Foundation
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The histone deacetylase inhibitor largazole 1 was synthesized by a convergent approach that involved several efficient and high yielding single pot multistep protocols. Initial attempts using tert-butyl as thiol protecting group proved problematic, and synthesis was accomplished by switching to the trityl protecting group. This synthetic protocol provides a convenient approach to many new largazole analogues. Three side chain analogues with multiple heteroatoms for chelation with Zn2+ were synthesized, and their biological activities were evaluated. They were less potent than largazole 1 in growth inhibition of HCT116 colon carcinoma cell line and in inducing increases in global H3 acetylation. Largazole 1 and the three side chain analogues had no effect on HDAC6, as indicated by the lack of increased acetylation of alpha-tubulin.
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