2. Academic Validation
  3. Design, synthesis and antimalarial/anticancer evaluation of spermidine linked artemisinin conjugates designed to exploit polyamine transporters in Plasmodium falciparum and HL-60 cancer cell lines

Design, synthesis and antimalarial/anticancer evaluation of spermidine linked artemisinin conjugates designed to exploit polyamine transporters in Plasmodium falciparum and HL-60 cancer cell lines

  • Bioorg Med Chem. 2010 Apr 1;18(7):2586-97. doi: 10.1016/j.bmc.2010.02.035.
James Chadwick 1,  Michael Jones,  Amy E Mercer,  Paul A Stocks,  Stephen A Ward,  B Kevin Park,  Paul M O'Neill
Affiliations

Affiliation

  • 1 Department of Chemistry, University of Liverpool, Liverpool L69 7ZD, UK.
PMID: 20227283 DOI: 10.1016/j.bmc.2010.02.035
Abstract

A series of artemisinin-spermidine conjugates designed to utilise the upregulated polyamine transporter found in Cancer cells have been prepared. These conjugates were evaluated against human promyelocytic leukaemia HL-60 cells and chloroquine-sensitive 3D7 Plasmodium falciparum and several show promising Anticancer and antimalarial activity. Although some limitations in this vector-based approach are apparent, a number of high potency Boc-protected analogues were identified with activity against malaria parasites as low as 0.21nM.

Figures