Semisynthesis of triptolide analogues: effect of γ-lactone and C-14 substituents on cytotoxic activities

  • Bioorg Med Chem Lett. 2011 May 15;21(10):3046-9. doi: 10.1016/j.bmcl.2011.03.025.
Yutaka Aoyagi  1 ,  Yukio Hitotsuyanagi ,  Tomoyo Hasuda ,  Haruhiko Fukaya ,  Koichi Takeya ,  Ritsuo Aiyama ,  Takeshi Matsuzaki ,  Shusuke Hashimoto
Affiliations
  • 1. School of Pharmacy, Tokyo University of Pharmacy & Life Sciences, 1432-1 Horinouchi, Hachioji, Tokyo 192-0392, Japan.
PMID: 21470864 DOI: 10.1016/j.bmcl.2011.03.025
Abstract

Triptolide γ-lactone and C-14 analogues were prepared and evaluated cytotoxity against human lung adenocarcinoma epithelial A549 cells and human colon adenocarcinoma HT-29 cells. γ-Lactone substructure and C-14 substituents affected the biological activities significantly.