synthesis and antiplasmodial evaluation of analogues based on the tricyclic core of thiaplakortones a–d
Clicks: 252
ID: 194839
2015
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.
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schwartz2015marinesynthesis
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| 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 |
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