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

Abstract：

: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.

journal_name

Bioorg Chem

journal_title

Bioorganic chemistry

authors

Yang H,Li Y,Chai H,Yakura T,Liu B,Yao Q

doi

10.1016/j.bioorg.2019.103369

subject

Has Abstract

pub_date

2020-05-01 00:00:00

pages

103369

eissn

0045-2068

issn

1090-2120

pii

S0045-2068(19)31138-1

journal_volume

98

pub_type

杂志文章

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