2. Academic Validation
  3. Synthesis and antitumor activities of quaternary carbon-containing selenolactones

Synthesis and antitumor activities of quaternary carbon-containing selenolactones

  • Bioorg Med Chem Lett. 2026 Feb 1:131:130439. doi: 10.1016/j.bmcl.2025.130439.
Danqing Li 1,  Yumiao Zhen 2,  Ran Tang 2,  Boying Wang 2,  Haijing Zhong 3,  Xiaojian Jiang 4,  Ying-Yeung Yeung 5
Affiliations

Affiliations

  • 1 First Affiliated Hospital of Guangzhou University of Traditional Chinese Medicine, Guangzhou 510405, China.
  • 2 State Key Laboratory of Bioactive Molecules and Druggability Assessment, Jinan University, Guangzhou 510632, China.
  • 3 State Key Laboratory of Bioactive Molecules and Druggability Assessment, Jinan University, Guangzhou 510632, China. Electronic address: hjzhong@jnu.edu.cn.
  • 4 State Key Laboratory of Bioactive Molecules and Druggability Assessment, Jinan University, Guangzhou 510632, China. Electronic address: chemjxj2015@jnu.edu.cn.
  • 5 Department of Chemistry and State Key Laboratory of Synthetic Chemistry, The Chinese University of Hong Kong, Shatin, NT, Hong Kong, China. Electronic address: yyyeung@cuhk.edu.hk.
PMID: 41120006 DOI: 10.1016/j.bmcl.2025.130439
Abstract

The cytotoxicity of α-exo-methylene-lactones has been extensively studied. However, further study of the α-exo-methylene-lactones for Anticancer application was hampered primarily by its poor selectivity and solubility. In the present work, a series of α-exo-methylene-selenolactone derivatives bearing amine substituent, selenium functionality and quaternary carbon center were synthesized and evaluated for their Anticancer activities. The most potent compound, 2d, was about 9-fold more selective for Cancer cells than normal cells. Moreover, 2d significantly inhibited tumor growth in mouse xenograft model and had no observable toxic effect.

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