期刊
ACS MEDICINAL CHEMISTRY LETTERS
卷 3, 期 9, 页码 749-753出版社
AMER CHEMICAL SOC
DOI: 10.1021/ml300162r
关键词
HDAC inhibitors; peptides; peptoids; macrocycles; apicidin
资金
- Benzon Foundation
- Lundbeck Foundation
- Danish Council for Independent Research \ Natural Sciences [10-080907]
- Skaggs Institute for Chemical Biology
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.
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