- Synthesis and proteasome inhibition of lithocholic acid derivatives.
Synthesis and proteasome inhibition of lithocholic acid derivatives.
Bioorganic & medicinal chemistry letters (2011-03-11)
Zhao Dang, Andrew Lin, Phong Ho, Dominique Soroka, Kuo-Hsiung Lee, Li Huang, Chin-Ho Chen
PMID21388808
RESUMEN
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 proteasome.
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