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Synthesis and proteasome inhibition of lithocholic acid derivatives |
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| Authors: | Dang Zhao Lin Andrew Ho Phong Soroka Dominique Lee Kuo-Hsiung Huang Li Chen Chin-Ho |
| Institution: | a Surgical Science, Department of Surgery, Duke University Medical Center, Durham, NC 27710, USA b Natural Products Research Laboratories, Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA c Chinese Medicine Research and Development Center, China Medical University and Hospital, Taichung 401, Taiwan |
| Abstract: | 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 noncompetitive inhibitors of the proteasome. |
| Keywords: | Lithocholic acid Proteasome Proteasome inhibitor |
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