期刊
JOURNAL OF ORGANIC CHEMISTRY
卷 85, 期 12, 页码 8253-8260出版社
AMER CHEMICAL SOC
DOI: 10.1021/acs.joc.0c00854
关键词
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资金
- NIH-AREA grant [1R15CA152869-01]
- NSF-TUES grant [1044396]
- Virginia's Commonwealth Health Research Board
- Research Corp [CC6250/5873]
- Camille and Henry Dreyfus Foundation [SU-04-007]
- Virginia Academy of Science
We describe the synthesis of Xyzidepsin, a depsipeptidic analogue of HDAC inhibitor Romidepsin (FK228), using a solid-phase strategy. Our latent thioester solid-phase linker was synthesized in 92% yield (three steps). Chemoselective conditions unmasked the thioester functionality and cyclized the depsipeptidic macrocycle. An IC50 value of 0.50 mu M +/- 0.05 was obtained for U937 cells. This synthetic route, well-suited to SAR, represents a generalizable route toward all manner of analogues, including structures with acidic and basic amino acids.
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