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  2. Modular Synthesis of Bioactive Selenoheterocycles for Efficient Cancer Therapy via Electrochemical Selenylation/Cyclization

Modular Synthesis of Bioactive Selenoheterocycles for Efficient Cancer Therapy via Electrochemical Selenylation/Cyclization

  • J Med Chem. 2025 Mar 27;68(6):6339-6360. doi: 10.1021/acs.jmedchem.4c02724.
Wenyan Xu 1 Chengwei Zheng 1 Mu Chen 1 Xin Deng 1 Lingmin Zhang 1 Xueping Lei 1 Lu Liang 1 Xiyong Yu 1 Xinwei Hu 1 Juyun He 1 Shuimu Lin 1 Zhixiong Ruan 1
Affiliations

Affiliation

  • 1 Guangzhou Municipal and Guangdong Provincial Key Laboratory of Molecular Target & Clinical Pharmacology, The State & NMPA Key Laboratory of Respiratory Disease, School of Pharmaceutical Sciences, Guangzhou Medical University, Guangzhou 511436, PR China.
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 4o, 5n, and 5o 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 5o was identified as the first inhibitor of DEAD-box helicase 10 (DDX10). An in vivo xenograft assay further confirmed the therapeutic potential of compound 5o, 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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