New betulinic acid derivatives as potent proteasome inhibitors

Keduo Qian, Sang Yong Kim, Hsin Yi Hung, Li Huang, Chin Ho Chen, Kuo Hsiung Lee

研究成果: Article同行評審

41 引文 斯高帕斯(Scopus)

摘要

In this study, 22 new betulinic acid (BA) derivatives were synthesized and tested for their inhibition of the chymotrypsin-like activity of 20S proteasome. From the SAR study, we concluded that the C-3 and C-30 positions are the pharmacophores for increasing the proteasome inhibition effects, and larger lipophilic or aromatic side chains are favored at these positions. Among the BA derivatives tested, compounds 13, 20, and 21 showed the best proteasome inhibition activity with IC 50 values of 1.42, 1.56, and 1.80 μM, respectively, which are three to fourfold more potent than the proteasome inhibition controls LLM-F and lactacystin.

原文English
頁(從 - 到)5944-5947
頁數4
期刊Bioorganic and Medicinal Chemistry Letters
21
發行號19
DOIs
出版狀態Published - 2011 10月 1

All Science Journal Classification (ASJC) codes

  • 生物化學
  • 分子醫學
  • 分子生物學
  • 藥學科學
  • 藥物發現
  • 臨床生物化學
  • 有機化學

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