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1.  Synthesis and proteasome inhibition of lithocholic acid derivatives 
A new class of proteasome inhibitors was synthesized using lithocholic acid as a scaffold. Modification at the C-3 position of lithocholic acid with a series of acid acyl groups yielded compounds with a range of potency on proteasome inhibition. Among them, the phenylene diacetic acid hemiester derivative (13) displayed the most potent proteasome inhibition with IC50 = 1.9 μM. Enzyme kinetic analysis indicates that these lithocholic acid derivatives are non-competitive inhibitors of the proteasome.
doi:10.1016/j.bmcl.2011.02.041
PMCID: PMC3072167  PMID: 21388808
Lithocholic acid; proteasome; proteasome inhibitor

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