dc.contributor.author |
Liew, Lydia |
en |
dc.contributor.author |
Kaiser, M |
en |
dc.contributor.author |
Copp, Brent |
en |
dc.coverage.spatial |
England |
en |
dc.date.accessioned |
2017-12-19T00:46:08Z |
en |
dc.date.available |
2012-11-14 |
en |
dc.date.issued |
2013-01-15 |
en |
dc.identifier.citation |
Bioorganic and Medicinal Chemistry Letters, 23(2):452-454, 15 Jan 2013 |
en |
dc.identifier.issn |
0960-894X |
en |
dc.identifier.uri |
http://hdl.handle.net/2292/36778 |
en |
dc.description.abstract |
Screening of synthesized and isolated marine natural products for in vitro activity against four parasitic protozoa has identified the ascidian metabolite 1,14-sperminedihomovanillamide (orthidine F, 1) as being a non-toxic, moderate growth inhibitor of Plasmodium falciparum (IC(50) 0.89 μM). Preliminary structure-activity relationship investigation identified essentiality of the spermine polyamine core and the requirement for 1,14-disubstitution for potent activity. One analogue, 1,14-spermine-di-(2-hydroxyphenylacetamide) (3), exhibited two orders of magnitude increased anti-P. f activity (IC(50) 8.6 nM) with no detectable in vitro toxicity. The ease of synthesis of phenylacetamido-polyamines, coupled with potent nM levels of activity towards dual drug resistant strains of P. falciparum makes this compound class of interest in the development of new antimalarial therapeutics. |
en |
dc.description.uri |
https://www.ncbi.nlm.nih.gov/pubmed/23265884 |
en |
dc.language |
English |
en |
dc.publisher |
Elsevier |
en |
dc.relation.ispartofseries |
Bioorganic and Medicinal Chemistry Letters |
en |
dc.rights |
Items in ResearchSpace are protected by copyright, with all rights reserved, unless otherwise indicated. Previously published items are made available in accordance with the copyright policy of the publisher. Details obtained from http://sherpa.ac.uk/romeo/issn/0960-894X/
https://www.elsevier.com/about/our-business/policies/sharing |
en |
dc.rights.uri |
https://researchspace.auckland.ac.nz/docs/uoa-docs/rights.htm |
en |
dc.subject |
Acetamides |
en |
dc.subject |
Animals |
en |
dc.subject |
Antimalarials |
en |
dc.subject |
Drug Discovery |
en |
dc.subject |
Inhibitory Concentration 50 |
en |
dc.subject |
Malaria |
en |
dc.subject |
Molecular Structure |
en |
dc.subject |
Plasmodium falciparum |
en |
dc.subject |
Spermine |
en |
dc.subject |
Structure-Activity Relationship |
en |
dc.title |
Discovery and preliminary structure-activity relationship analysis of 1,14-sperminediphenylacetamides as potent and selective antimalarial lead compounds |
en |
dc.type |
Journal Article |
en |
dc.identifier.doi |
10.1016/j.bmcl.2012.11.072 |
en |
pubs.issue |
2 |
en |
pubs.begin-page |
452 |
en |
pubs.volume |
23 |
en |
dc.rights.holder |
Copyright: Elsevier |
en |
dc.identifier.pmid |
23265884 |
en |
pubs.author-url |
http://www.sciencedirect.com/science/article/pii/S0960894X12015247 |
en |
pubs.end-page |
454 |
en |
pubs.publication-status |
Published |
en |
dc.rights.accessrights |
http://purl.org/eprint/accessRights/RestrictedAccess |
en |
pubs.subtype |
Article |
en |
pubs.elements-id |
370864 |
en |
pubs.org-id |
Medical and Health Sciences |
en |
pubs.org-id |
Medical Sciences |
en |
pubs.org-id |
Auckland Cancer Research |
en |
pubs.org-id |
Science |
en |
pubs.org-id |
Chemistry |
en |
pubs.org-id |
Science Research |
en |
pubs.org-id |
Maurice Wilkins Centre (2010-2014) |
en |
dc.identifier.eissn |
1464-3405 |
en |
dc.identifier.pii |
S0960-894X(12)01524-7 |
en |
pubs.record-created-at-source-date |
2017-12-19 |
en |
pubs.online-publication-date |
2012-11-29 |
en |
pubs.dimensions-id |
23265884 |
en |