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Molecules 2014, 19(2), 2213-2225; doi:10.3390/molecules19022213

Synthesis of ∆3-2-Hydroxybakuchiol Analogues and Their Growth Inhibitory Activity against Rat UMR106 Cells

1, 1, 1, 1, 2,*  and 1,3,*
1 School of Pharmacy, Fudan University, Shanghai 201203, China 2 Department of Pharmaceutical Botany, School of Pharmacy, Second Military Medical University, Shanghai 200433, China 3 Key Laboratory of Synthetic Chemistry of Natural Substances, Shanghai Institute of Organic Chemistry, Chinese Academy of Sciences, Shanghai 200032, China
* Authors to whom correspondence should be addressed.
Received: 17 January 2014 / Revised: 9 February 2014 / Accepted: 11 February 2014 / Published: 20 February 2014
(This article belongs to the Section Medicinal Chemistry)
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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.
Keywords: bakuchiol; natural product analogues; cytotoxic activity bakuchiol; natural product analogues; cytotoxic activity
This is an open access article distributed under the Creative Commons Attribution License (CC BY 3.0).

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Zhao, Q.; Xu, Q.; Shan, G.; Dong, C.; Zhang, H.; Lei, X. Synthesis of ∆3-2-Hydroxybakuchiol Analogues and Their Growth Inhibitory Activity against Rat UMR106 Cells. Molecules 2014, 19, 2213-2225.

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