Synthesis and biological evaluation of 2-epi-jaspine B analogs as selective sphingosine kinase 1 inhibitors

Haoran Yang, Ying Li, Huining Chai, Takayuki Yakura, Bo Liu*, Qingqiang Yao

*この論文の責任著者

研究成果: ジャーナルへの寄稿学術論文査読

16 被引用数 (Scopus)

抄録

2-Epi-jaspine B is an isomer of the natural product jaspine B and shows certain selectivity for SphK1 and potent antitumor activity. Based on the crystal structure of SphK1, we transformed the structure of 2-epi-jaspine B and modified the hydrophobic side chain to obtain a series of 2-epi-jaspine B analogs. The MTT assay was used to examine the antitumor activities of these analogs. We identified a novel 2-epi-jaspine B analog YHR17, which has potent antiproliferative activities for tested cell lines with IC50 values that ranged from 0.68 to 5.68 μM and inhibited the proliferation of the A375 cell line by affecting the cell cycle and apoptosis. Furthermore, YHR17 inhibited SphK1 with more than 125-fold selectivity over SphK2.

本文言語英語
論文番号103369
ジャーナルBioorganic Chemistry
98
DOI
出版ステータス出版済み - 2020/05

ASJC Scopus 主題領域

  • 生化学
  • 分子生物学
  • 創薬
  • 有機化学

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