Marine Drugs · 2017 · 38 citations · 20 references
PharmacyMedicinal ChemistryPharmacologyDrug DiscoveryOrganic ChemistrySynthetic Medicinal ChemistryEnzyme InhibitionNatural Product Drug DiscoveryStructure-activity Relationship AnalysisBioactive Compounds From Marine SpongesBiological Activity FeaturesIndole AlkaloidsIndole ChemistryMarine Sponge MetabolitesPlant AlkaloidsPlasmodium FalciparumSponges As Drug Sources
A deep-water sponge of the genus Spongosorites has yielded a bis-indole alkaloid which we have named dragmacidin G. Dragmacidin G was first reported by us in the patent literature and has recently been reported by Hitora et al. from a sponge of the genus Lipastrotheya. Dragmacidin G is the first in this series of compounds to have a pyrazine ring linking the two indole rings. It also has a rare N-(2-mercaptoethyl)-guanidine side chain. Dragmacidin G shows a broad spectrum of biological activity including inhibition of methicillin-resistant Staphylococcus aureus, Mycobacterium tuberculosis, Plasmodium falciparum, and a panel of pancreatic cancer cell lines.
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Shinji Tsujii, Kenneth L. Rinehart, Sarath P. Gunasekera et al. · The Journal of Organic Chemistry · 1988 · 154 citations