Synthesis and cytotoxic evaluation of halogenated α-exo-methylene-lactones

  • Bioorg Med Chem. 2020 Feb 1;28(3):115281. doi: 10.1016/j.bmc.2019.115281.
Haoquan He  1 ,  Zheng Liu  2 ,  Wei Wang  1 ,  Xiaojian Jiang  3
Affiliations
  • 1. International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), College of Pharmacy, Jinan University, Guangzhou 510632, China.
  • 2. Foshan Stomatology Hospital, School of Stomatology and Medicine, Foshan University, Foshan 528000, China.
  • 3. International Cooperative Laboratory of Traditional Chinese Medicine Modernization and Innovative Drug Development of Chinese Ministry of Education (MOE), College of Pharmacy, Jinan University, Guangzhou 510632, China. Electronic address: [email protected].
PMID: 31889606 DOI: 10.1016/j.bmc.2019.115281
Abstract

α-exo-Methylene-γ-butyrolactones and α-exo-methylene-δ-valerolactones constitute an important group of natural and bioactive products. A simple and general protocol of halolactonization of dienoic acids to obtain various α-exo-methylene-lactones in excellent yields is described. The resulting halogenated α-exo-methylene-lactones were found to exhibit potent cytotoxic activities.

Keywords
Cytotoxic activity; Dienoic acid; Halolactonization; α-exo-methylene-lactones.