Abstract
A series of ∆3-2-hydroxybakuchiol analogues have been synthesized and tested for their growth inhibitory activity against rat UMR106 cells by using the MTT method. Some of them exhibit enhanced activities compared with the natural product, and the preliminary SAR profile shows that the chain tail on the natural product could be subtly modified to enhance the activity and the aromatic moiety or the terminal olefin on the main chain can also be modified without any evident loss of activity. The stereo-configuration of the quaternary chiral center has an important influence on the activity.
Highlights
Natural products from plants are an important source of potential therapeutic agents for human health
A facile asymmetric synthesis of ∆3-2-hydroxybakuchiol was established and the compound was tested for antiosteoporosis effects [31,32]
This natural product did not show the desired activity, but it exhibited growth inhibitory activity against osteosarcoma cells with an IC50 value of 69 μM, suggesting that it was worthy of further investigation [33]
Summary
Natural products from plants are an important source of potential therapeutic agents for human health. To the best of our knowledge, only Guo and co-workers have recently investigated its inhibitory effects against monoamine transporters, suggesting that it might be a potential psychopharmacologic agent for the treatment of psychogenic disorders [26]. A facile asymmetric synthesis of ∆3-2-hydroxybakuchiol was established and the compound was tested for antiosteoporosis effects [31,32]. This natural product did not show the desired activity, but it exhibited growth inhibitory activity against osteosarcoma cells (rat UMR106 cell) with an IC50 value of 69 μM, suggesting that it was worthy of further investigation [33]. We would replace the terminal olefin with an ethyl moiety (R2) in order to probe the effect of this moiety on the activity (Figure 1)
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