{"status":"ok","message-type":"work","message-version":"1.0.0","message":{"indexed":{"date-parts":[[2026,10,5]],"date-time":"2026-10-05T19:47:06Z","timestamp":1791229626834,"version":"4.1.0"},"reference-count":32,"publisher":"MDPI AG","issue":"6","license":[{"start":{"date-parts":[[2014,5,28]],"date-time":"2014-05-28T00:00:00Z","timestamp":1401235200000},"content-version":"vor","delay-in-days":0,"URL":"https:\/\/creativecommons.org\/licenses\/by\/3.0\/"}],"content-domain":{"domain":[],"crossmark-restriction":false},"short-container-title":["Marine Drugs"],"abstract":"<jats:p>Pure compound screening has previously identified the indolglyoxy lamidospermidine ascidian metabolites didemnidine A and B (2 and 3) to be weak growth inhibitors of Trypanosoma brucei rhodesiense (IC50 59 and 44 \u03bcM, respectively) and Plasmodium falciparum (K1 dual drug resistant strain) (IC50 41 and 15 \u03bcM, respectively), but lacking in selectivity (L6 rat myoblast, IC50 24 \u03bcM and 25 \u03bcM, respectively).  To expand the structure\u2013activity relationship of this compound class towards both parasites, we have prepared and biologically tested a library of analogues that includes indoleglyoxyl and indoleacetic \u201ccapping acids\u201d, and polyamines including spermine  (PA3-4-3) and extended analogues PA3-8-3 and PA3-12-3. 7-Methoxy substituted indoleglyoxylamides were typically found to exhibit the most potent antimalarial activity (IC50 10\u201392 nM) but with varying degrees of selectivity versus the L6 rat myoblast cell line. A 6-methoxyindolglyoxylamide analogue was the most potent growth inhibitor of  T. brucei (IC50 0.18 \u03bcM) identified in the study: it, however, also exhibited poor selectivity (L6 IC50 6.0 \u03bcM). There was no apparent correlation between antimalarial and  anti-T. brucei activity in the series. In vivo evaluation of one analogue against Plasmodium berghei was undertaken, demonstrating a modest 20.9% reduction in parasitaemia.<\/jats:p>","DOI":"10.3390\/md12063138","type":"journal-article","created":{"date-parts":[[2014,5,28]],"date-time":"2014-05-28T11:10:36Z","timestamp":1401275436000},"page":"3138-3160","update-policy":"https:\/\/doi.org\/10.3390\/mdpi_crossmark_policy","source":"Crossref","is-referenced-by-count":21,"title":["Investigation of Indolglyoxamide and Indolacetamide Analogues of Polyamines as Antimalarial and Antitrypanosomal Agents"],"prefix":"10.3390","volume":"12","author":[{"given":"Jiayi","family":"Wang","sequence":"first","affiliation":[{"name":"School of Chemical Sciences, University of Auckland, Private Bag 92019, Auckland 1142,  New Zealand"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"given":"Marcel","family":"Kaiser","sequence":"additional","affiliation":[{"name":"Swiss Tropical and Public Health Institute, Socinstrasse 57, PO Box, Basel CH-4002, Switzerland"},{"name":"University of Basel, Basel CH-4003, Switzerland"}],"role":[{"vocabulary":"crossref","role":"author"}]},{"ORCID":"https:\/\/orcid.org\/0000-0001-5492-5269","authenticated-orcid":false,"given":"Brent","family":"Copp","sequence":"additional","affiliation":[{"name":"School of Chemical Sciences, University of Auckland, Private Bag 92019, Auckland 1142,  New Zealand"}],"role":[{"vocabulary":"crossref","role":"author"}]}],"member":"1968","published-online":{"date-parts":[[2014,5,28]]},"reference":[{"key":"ref_1","doi-asserted-by":"crossref","first-page":"647","DOI":"10.1039\/b413742f","article-title":"Polyamine alkaloids","volume":"22","author":"Bienz","year":"2005","journal-title":"Nat. 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