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.

Chadwick, James, Jones, Michael, Mercer, Amy E, Stocks, Paul A., Ward, Stephen ORCID: https://orcid.org/0000-0003-2331-3192, Park, B Kevin and O'Neill, Paul M (2010) '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.'. Bioorganic and Medicinal Chemistry, Vol 18, Issue 7, pp. 2586-97.

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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.

Item Type:	Article
Subjects:	QV Pharmacology > Anti-Inflammatory Agents. Anti-Infective Agents. Antineoplastic Agents > QV 256 Antimalarials QV Pharmacology > QV 34 Experimental pharmacology (General)
Digital Object Identifer (DOI):	https://doi.org/10.1016/j.bmc.2010.02.035
Related URLs:	Publisher
Depositing User:	Mary Creegan
Date Deposited:	31 Aug 2010 11:23
Last Modified:	08 Jun 2018 11:11
URI:	https://archive.lstmed.ac.uk/id/eprint/1019

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