Abstract
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.
| Original language | English |
|---|---|
| Journal | ACS Medicinal Chemistry Letters |
| Volume | 3 |
| Issue number | 9 |
| Pages (from-to) | 749-753 |
| ISSN | 1948-5875 |
| DOIs | |
| Publication status | Published - 2012 |
UN SDGs
This output contributes to the following UN Sustainable Development Goals (SDGs)
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SDG 3 Good Health and Well-being
Keywords
- HDAC inhibitors
- Peptides
- Peptoids
- Macrocycles
- Apicidin
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