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
  • 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: [email protected].
  • 4. State Key Laboratory of Bioactive Molecules and Druggability Assessment, Jinan University, Guangzhou 510632, China. Electronic address: [email protected].
  • 5. Department of Chemistry and State Key Laboratory of Synthetic Chemistry, The Chinese University of Hong Kong, Shatin, NT, Hong Kong, China. Electronic address: [email protected].
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.

Products