synthesis and antiplasmodial evaluation of analogues based on the tricyclic core of thiaplakortones a–d

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ID: 194839
2015
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Abstract
Six regioisomers associated with the tricyclic core of thiaplakortones A–D have been synthesized. Reaction of 1H-indole-4,7-dione and 1-tosyl-1H-indole-4,7-dione with 2-aminoethanesulfinic acid afforded a regioisomeric series, which was subsequently deprotected and oxidized to yield the tricyclic core scaffolds present in the thiaplakortones. All compounds were fully characterized using NMR and MS data. A single crystal X-ray structure was obtained on one of the N-tosyl derivatives. All compounds were screened for in vitro antiplasmodial activity against chloroquine-sensitive (3D7) and multidrug-resistant (Dd2) Plasmodium falciparum parasite lines. Several analogues displayed potent inhibition of P. falciparum growth (IC50 < 500 nM) but only moderate selectivity for P. falciparum versus human neonatal foreskin fibroblast cells.
Reference Key
schwartz2015marinesynthesis Use this key to autocite in the manuscript while using SciMatic Manuscript Manager or Thesis Manager
Authors ;Brett D. Schwartz;Mark J. Coster;Tina S. Skinner-Adams;Katherine T. Andrews;Jonathan M. White;Rohan A. Davis
Journal jixie gongcheng xuebao/journal of mechanical engineering
Year 2015
DOI
10.3390/md13095784
URL
http://www.mdpi.com/1660-3397/13/9/5784
Keywords
synthesis plasmodium falciparum crystal antiplasmodial cytotoxicitybiology (general)

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