Synthesis of 10-substituted triazolyl artemisinins possessing anticancer activity via Huisgen 1,3-dipolar cylcoaddition

  • Bioorg Med Chem Lett. 2009 Jan 15;19(2):382-5. doi: 10.1016/j.bmcl.2008.11.067.
Sungsik Cho  1 ,  Sangtae Oh ,  Yumi Um ,  Ji-Hee Jung ,  Jungyeob Ham ,  Woon-Seob Shin ,  Seokjoon Lee
Affiliations
  • 1. Department of Basic Science, Kwandong University College of Medicine, 522 Naegok, Gangneung , Gangwon 210-701, Republic of Korea.
PMID: 19081249 DOI: 10.1016/j.bmcl.2008.11.067
Abstract

Most of the 10-substituted triazolylartemisinin synthesized via the Huisgen 1,3-dipolar cylcoaddition of diastereomeric 10-azidoartemisinin (5, 6, and 7) with various alkynes (a-h) exhibit strong growth inhibition activity, even at sub-micromolar concentrations, against various Cancer cell lines such as DLD-1, U-87, Hela, SiHa, A172, and B16. In particular, 10b and 10f showed a highly strong cytotoxicity.