title: 3-Nitro-2H-chromenes as a new class of inhibitors against thioredoxin reductase and proliferation of cancer cells.
abstract: 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.
authors: School of Pharmaceutical Sciences, Sun Yat-sen University, Guangzhou, China.
authors: Guo-Qiang
authors: GQ
authors: Xiao
authors: Bao-Xia
authors: BX
authors: Liang
authors: Shu-Han
authors: SH
authors: Chen
authors: Tian-Miao
authors: TM
authors: Ou
authors: Xian-Zhang
authors: XZ
authors: Bu
authors: Ming
authors: M
authors: Yan
mesh_terms: D001578:Benzopyrans / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D045744:Cell Line, Tumor; D049109:Cell Proliferation / Q000187:drug effects; D004791:Enzyme Inhibitors / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D009574:Nitro Compounds / Q000138:chemical synthesis / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship; D013880:Thioredoxin-Disulfide Reductase / Q000037:antagonists & inhibitors*
chemical_list: D001578:Benzopyrans; D004791:Enzyme Inhibitors; D009574:Nitro Compounds; D013880:Thioredoxin-Disulfide Reductase