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DRUG:

spliceostatin A (SSA)

i
Other names: SSA
Company:
Riken
Drug class:
SF3B1 inhibitor, RNA splicing modulator
over1year
Design and synthesis of 4-acetoxypentanamide derivatives of spliceostatin A and their biological evaluation towards prostate cancer treatment. (PubMed, Bioorg Med Chem Lett)
We designed and synthesized novel 4-acetoxypentanamide derivatives of spliceostatin A, whose 4-acetoxypentenamide moiety is reduced (7), isomerized (8), or substituted with methyl at the α-position (9). The results of biological evaluation against AR-V7 and the docking analysis of each derivative suggest that the geometry of the 4-acetoxypentenamide moiety of spliceostatin A is important for its biological activity.
Journal
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AR (Androgen receptor)
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AR splice variant 7
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spliceostatin A (SSA)