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3‐Nitro‐2 H ‐chromenes as a New Class of Inhibitors against Thioredoxin Reductase and Proliferation of Cancer Cells
Author(s) -
Xiao GuoQiang,
Liang BaoXia,
Chen ShuHan,
Ou TianMiao,
Bu XianZhang,
Yan Ming
Publication year - 2012
Publication title -
archiv der pharmazie
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.468
H-Index - 61
eISSN - 1521-4184
pISSN - 0365-6233
DOI - 10.1002/ardp.201200121
Subject(s) - pharmacophore , thioredoxin reductase , thioredoxin , chemistry , inhibitory postsynaptic potential , structure–activity relationship , reductase , nitro , cell growth , cancer cell , stereochemistry , enzyme , biochemistry , cancer , in vitro , biology , genetics , alkyl , organic chemistry , neuroscience
A series of 3‐nitrochromenes were designed and synthesized. These compounds showed good inhibitory activity against thioredoxin reductase (TrxR) and the proliferation of A549 cancer cells. The structure–activity relationship analysis indicates that the 3‐nitrochromene scaffold is the crucial pharmacophore for achieving good inhibitory activity. The bromo‐substitutions at the 6‐ and 8‐position of 3‐nitrochromene significantly increase the inhibitory activity.