Macrocyclic Peptoid–Peptide Hybrids as Inhibitors of Class I Histone Deacetylases
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https://figshare.com/articles/dataset/Macrocyclic_Peptoid_Peptide_Hybrids_as_Inhibitors_of_Class_I_Histone_Deacetylases/2487163
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资源简介：
We report the design, synthesis, and biological evaluation
of the
first macrocyclic peptoid-containing histone deacetylase (HDAC) inhibitors.
The compounds selectively inhibit human class I HDAC isoforms in vitro,
with no inhibition of the tubulin deacetylase activity associated
with class IIb HDAC6 in cultured Jurkat cells. Compared to the natural
product apicidin (1), one inhibitor (compound 10) showed equivalent potency against K-562 cells, but was more cytoselective
across a panel of cancer cell lines.
创建时间：
2012-09-13
