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

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

Affiliation

  • 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.

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