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Synthesis and proteasome inhibition of lithocholic acid derivatives.
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ABSTRACT:
SUBMITTER: Dang Z
PROVIDER: S-EPMC3072167 | biostudies-literature | 2011 Apr
REPOSITORIES: biostudies-literature
Publications
Synthesis and proteasome inhibition of lithocholic acid derivatives.
Bioorganic & medicinal chemistry letters 20110217 7
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 IC(50) = 1.9 μM. Enzyme kinetic analysis indicates that these lithocholic acid derivatives are noncompetitive inhibitors of the proteas ...[more]