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Molecules 2014, 19(2), 2213-2225;

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

School of Pharmacy, Fudan University, Shanghai 201203, China
Department of Pharmaceutical Botany, School of Pharmacy, Second Military Medical University, Shanghai 200433, China
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. View Full-Text
Keywords: bakuchiol; natural product analogues; cytotoxic activity bakuchiol; natural product analogues; cytotoxic activity

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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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