title: Synthesis of ∆3-2-hydroxybakuchiol analogues and their growth inhibitory activity against rat UMR106 cells.
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.
authors.affiliation: School of Pharmacy, Fudan University, Shanghai 201203, China.
authors.forename: Qun
authors.initials: Q
authors.lastname: Zhao
authors.affiliation: School of Pharmacy, Fudan University, Shanghai 201203, China.
authors.forename: Qianqian
authors.initials: Q
authors.lastname: Xu
authors.affiliation: School of Pharmacy, Fudan University, Shanghai 201203, China.
authors.forename: Guangsheng
authors.initials: G
authors.lastname: Shan
authors.affiliation: School of Pharmacy, Fudan University, Shanghai 201203, China.
authors.forename: Chao
authors.initials: C
authors.lastname: Dong
authors.affiliation: Department of Pharmaceutical Botany, School of Pharmacy, Second Military Medical University, Shanghai 200433, China. zhanghong@smmu.edu.cn.
authors.forename: Hong
authors.initials: H
authors.lastname: Zhang
authors.affiliation: School of Pharmacy, Fudan University, Shanghai 201203, China. leixs@fudan.edu.cn.
authors.forename: Xinsheng
authors.initials: X
authors.lastname: Lei
mesh_terms: D000818:Animals; D002455:Cell Division / Q000187:drug effects*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects*; D010636:Phenols / Q000737:chemistry / Q000494:pharmacology*; D020836:Protein Structure, Quaternary; D051381:Rats; D013329:Structure-Activity Relationship
chemical_list: D010636:Phenols; C542038:delta(3),2-hydroxybakuchiol