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.
journal_name
Mar Drugsjournal_title
Marine drugsauthors
Schwartz BD,Coster MJ,Skinner-Adams TS,Andrews KT,White JM,Davis RAdoi
10.3390/md13095784subject
Has Abstractpub_date
2015-09-15 00:00:00pages
5784-95issue
9issn
1660-3397pii
md13095784journal_volume
13pub_type
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