Modular Synthesisof Bioactive Selenoheterocyclesfor Efficient Cancer Therapy via Electrochemical Selenylation/Cyclization

A green, efficient, and environmentally friendly electrochemical strategy was developed for synthesizing a series of selenoheterocyclic compounds. The antitumor activities of these compounds were evaluated, revealing that compounds <b>4o</b>, <b>5n</b>, and <b>5o</b> demonstrated remarkable antitumor efficacy. These compounds effectively inhibited lung cancer by inducing cell apoptosis, causing DNA damage, and suppressing the progression of epithelial–mesenchymal transition. Notably, compound <b>5o</b> was identified as the first inhibitor of DEAD-box helicase 10 (DDX10). An <i>in vivo</i> xenograft assay further confirmed the therapeutic potential of compound <b>5o</b>, demonstrating tumor growth inhibition rates of 60%, 78%, and 88% at doses of 5 mg/kg, 10 mg/kg, and 20 mg/kg, respectively. This study highlights a promising chemotherapeutic agent for the effective treatment of lung cancer.

Publication Details

Journal
Figshare
Published
2025-03-10
DOI
https://doi.org/10.1021/acs.jmedchem.4c02724.s001
Primary Topic
Organoselenium and organotellurium chemistry
Type
article
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article

Modular Synthesisof Bioactive Selenoheterocyclesfor Efficient Cancer Therapy via Electrochemical Selenylation/Cyclization

Figshare
Organoselenium and organotellurium chemistry
article

Modular Synthesisof Bioactive Selenoheterocyclesfor Efficient Cancer Therapy via Electrochemical Selenylation/Cyclization

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Abstract

A green, efficient, and environmentally friendly electrochemical strategy was developed for synthesizing a series of selenoheterocyclic compounds. The antitumor activities of these compounds were evaluated, revealing that compounds <b>4o</b>, <b>5n</b>, and <b>5o</b> demonstrated remarkable antitumor efficacy. These compounds effectively inhibited lung cancer by inducing cell apoptosis, causing DNA damage, and suppressing the progression of epithelial–mesenchymal transition. Notably, compound <b>5o</b> was identified as the first inhibitor of DEAD-box helicase 10 (DDX10). An <i>in vivo</i> xenograft assay further confirmed the therapeutic potential of compound <b>5o</b>, demonstrating tumor growth inhibition rates of 60%, 78%, and 88% at doses of 5 mg/kg, 10 mg/kg, and 20 mg/kg, respectively. This study highlights a promising chemotherapeutic agent for the effective treatment of lung cancer.

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Organoselenium and organotellurium chemistry
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