title: Synthesis and decreasing Aβ content evaluation of arctigenin-4-yl carbamate derivatives.
abstract: A series of arctigenin-4-yl carbamate derivatives were synthesized and evaluated for potency in reducing β-amyloid (Aβ) content in HEK293-APPswe cells. Most of the arctigenin-4-yl aralkyl or aryl carbamate derivatives showed improved potency in reducing Aβ content. Among the synthesized compounds, arctigenin-4-yl (3-chlorophenyl)carbamate (20) exhibited the strongest potency with 78.7% Aβ content reduction at 20μM. Furthermore, the effect of arctigenin-4-yl (4-chlorophenyl)carbamate (19) and arctigenin-4-yl (3-chlorophenyl)carbamate (20) on lowing Aβ content was better than arctigenin under the concentrations of 1, 10 and 20μM.
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, PR China.
authors.forename: Xingyu
authors.initials: X
authors.lastname: Xu
authors.affiliation: School of Life Science, Shanghai University, 99 Shangda Road, Shanghai 200444, PR China.
authors.forename: Cong
authors.initials: C
authors.lastname: Li
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, PR China. Electronic address: mlei@simm.ac.cn.
authors.forename: Min
authors.initials: M
authors.lastname: Lei
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, PR China.
authors.forename: Zhiyuan
authors.initials: Z
authors.lastname: Zhu
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, PR China.
authors.forename: Jianming
authors.initials: J
authors.lastname: Yan
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, PR China; School of Life Science, Shanghai University, 99 Shangda Road, Shanghai 200444, PR China. Electronic address: xshen@simm.ac.cn.
authors.forename: Xu
authors.initials: X
authors.lastname: Shen
authors.affiliation: State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, University of Chinese Academy of Sciences, Chinese Academy of Sciences, Shanghai 201203, PR China. Electronic address: lhhu@simm.ac.cn.
authors.forename: Lihong
authors.initials: L
authors.lastname: Hu
mesh_terms: D016229:Amyloid beta-Peptides / Q000378:metabolism*; D002219:Carbamates / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D005663:Furans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D057809:HEK293 Cells; D006801:Humans; D017705:Lignans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D016229:Amyloid beta-Peptides; D002219:Carbamates; D005663:Furans; D017705:Lignans; C000621095:arctigenin-4-yl (3-chlorophenyl)carbamate; C000621094:arctigenin-4-yl (4-chlorophenyl)carbamate; C071942:arctigenin
keywords: Alzheimer’s disease (AD); Arctigenin (ATG); Arctigenin-4-yl 3-carbamate; Natural product; Structure–activity relationships (SARs)