Journal
ACS MEDICINAL CHEMISTRY LETTERS
Volume 11, Issue 6, Pages 1310-1315Publisher
AMER CHEMICAL SOC
DOI: 10.1021/acsmedchemlett.0c00153
Keywords
Prostate cancer; splicing; splicing variant; spliceostatin A; toxicity
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Funding
- JSPS KAKENHI [JP A16H010260, 18H04260, A262880510, T15K149760, T15KT00630]
- Platform Project for Supporting Drug Discovery and Life Science Research (Basis for Supporting Innovative Drug Discovery and Life Science Research (BINDS)) from the AMED [JP19am0101084]
- Shorai Foundation for Science and Technology
- Grants-in-Aid for Scientific Research [18H04260] Funding Source: KAKEN
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We designed and synthesized a novel 1,2-deoxy-pyranose and terminal epoxide methyl substituted derivatives of spliceostatin A using Julia-Kocienski olefination as a key step. With respect to the biological activity, the 1,2-deoxy-pyranose analogue of spliceostatin A suppressed AR-V7 expression at the nano level (IC50 = 3.3 nM). In addition, the in vivo toxicity test showed that the 1,2-deoxy-pyranose analogue was able to avoid severe toxicity compared to spliceostatin A.
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