Related Experiment Video
Updated: Jan 17, 2026

Functionalized Spirocyclic Heterocycle Synthesis and Cytotoxicity Assay
Published on: February 9, 2021
Structural Optimization of Dithiaarsanes-Enhanced Cytotoxicity to Leukemia Cells With Improved Thioredoxin Reductase
Linjie Zhang1,2, Jintao Zhao2,3, Meirong Yi2
1School of Chemistry and Chemical Engineering, Nanjing University of Science & Technology, Nanjing, Jiangsu, China.
None:
Herein, we report the rational design and optimization of dithiaarsane-based organoarsenicals that target thioredoxin reductase (TrxR), a selenoenzyme essential for maintaining cellular redox balance and often upregulated in various cancers. Guided by structure-activity relationship (SAR) analysis, refinement of the arsenic-sulfur heterocyclic scaffold afforded compound 37, which exhibits potent cytotoxicity against HL-60 leukemia cells. Mechanistic studies revealed that compound 37 efficiently inhibits TrxR activity, increases intracellular reactive oxygen species, and triggers apoptosis. Collectively, these results, together with the chemically versatile dithiaarsane scaffold established herein, provide a solid foundation for the development of next-generation TrxR-targeted therapeutics and redox-responsive functional molecules.
Related Concept Videos
Aryldiazonium Salts to Azo Dyes: Diazo Coupling
Preparation and Reactions of Thiols
Electron Transport Chain: Complex I and II
ROS generation is regulated and maintained at moderate levels necessary...
Diels–Alder Reaction: Characteristics of Dienes
Characteristics of the diene
Conformation
The simplest example of a diene is 1,3-butadiene, an acyclic conjugated π system. At room temperature, the molecule exists as a mixture of s-cis and s-trans conformers by virtue of rotation around the carbon–carbon single bond. Although the s-trans isomer is more stable,...
Nucleophilic Aromatic Substitution of Aryldiazonium Salts: Aromatic SN1
In the Sandmeyer reaction, for example, the diazonio group is replaced by a chloro, bromo,...

