Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents.
Synthesis and biological evaluation of piperlongumine derivatives as potent anti-inflammatory agents.
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DOI：
10.1016/j.bmcl.2014.10.054
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发表时间：
2014-12
影响因子：
2.7
通讯作者：
Y. Seo;Jin-Kyung Kim;J. Jun
中科院分区：
文献类型：
--
作者：
Y. Seo;Jin-Kyung Kim;J. Jun
Piperlongumine (PL) and its derivatives were synthesized by the direct reaction between acid chloride of 3,4,5-trimethoxycinnamic acid and various amides/lactams. Later their anti-inflammatory effects were evaluated in lipopolysaccharide (LPS)-induced RAW-264.7 macrophages. Of the piperlogs prepared in this study, the maximum (91%) inhibitory activity was observed with PL (IC50= 3 μM) but showed cytotoxicity whereas compound3(IC50= 6 μM) which possess α,β-unsaturated γ-butyrolactam moiety offered good level (65%) of activity with no cytotoxicity. This study revealed that amide/lactam moiety connected to cinnamoyl group with minimum 3 carbon chain length and α,β-unsaturation is fruitful to show potent anti-inflammatory activity.
