Synthesis and proteasome inhibition of lithocholic acid derivatives

Z Dang, A Lin, P Ho, D Soroka, KH Lee, L Huang…

文献索引：Dang, Zhao; Lin, Andrew; Ho, Phong; Soroka, Dominique; Lee, Kuo-Hsiung; Huang, Li; Chen, Chin-Ho Bioorganic and Medicinal Chemistry Letters, 2011 , vol. 21, # 7 p. 1926 - 1928

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被引用次数: 10

摘要

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 ...