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Highly Efficient Synthesis and Structure–Activity Relationships of a Small Library of Substituted 1,4‐Naphthoquinones
Author(s) -
Bao Na,
Ou Jinfeng,
Shi Wei,
Li Na,
Chen Li,
Sun Jianbo
Publication year - 2018
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201800207
Subject(s) - plumbagin , chemistry , combinatorial chemistry , naphthoquinone , stereochemistry , structure–activity relationship , organic chemistry , biochemistry , in vitro , genetics , biology
A platform of highly efficient synthetic methodologies has been established to access a focused library of substituted 1,4‐naphthoquinones derivatives functionalized with a diversity of amino/hydroxy/alkyl groups. Furthermore, the structure–activity relationship deduced from antiproliferative activities and toxicities of this 1,4‐naphthoquinone library and intracellular reactive oxygen species (ROS) level detections might warrant future potential of plumbagin ( 2 ) and compound 13 as promising basic structures to develop novel anti‐cancer agents.