科研之友
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摘要
In our previous study, selaginpulvilins A-D (1-4) featuring an unprecedented 9,9-diphenyl-1-(phenylethynyl)- 9H-fluorene skeleton were identified as potent phosphodiesterase-4 (PDE4) inhibitors from Selaginella pulvinata. In the current work, a large-scale reinvestigation of the same plant led to the isolation of six additional new analogues, selaginpulvilins E-J (5-10), among which 5 features a rare 6(4-hydroxyphenyl)-2H-pyran-2-one unit. Compounds 5-10 exhibited remarkable inhibitory activities against PDE4 with IC50 values in the range of 0.22-1.38 mu M. The first total synthesis of selaginpulvilins A-F (1-6) was developed in 7-11 steps involving a Friedel-Crafts reaction as the key reaction, which provides a feasible access to this scaffold.
- 出版日期2017-2-1
- 单位中山大学
