ArticleMarine drugs2009
Antiplasmodial activities of homogentisic acid derivative protein kinase inhibitors isolated from a Vanuatu marine sponge Pseudoceratina sp.
Article in Marine drugs, 2009. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 16 papers.
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Who cites it
16 citing papers in PubMed, 39 citations in OpenAlex.
- Potential of Marine Sponge Metabolites against Prions: Bromotyrosine Derivatives, a Family of Interest.Marine drugs · 2024Article
- Marine organisms as potential sources of natural products for the prevention and treatment of malaria.RSC advances · 2023Review
- Psammaplysins: Insights from Natural Sources, Structural Variations, and Pharmacological Properties.Marine drugs · 2022Review
- Application of Networking Approaches to Assess the Chemical Diversity, Biogeography, and Pharmaceutical Potential of Verongiida Natural Products.Marine drugs · 2021Article
- Bioactive Bromotyrosine Derivatives from the Pacific Marine SpongeMarine drugs · 2021Article
- An Update on Development of Small-Molecule Plasmodial Kinase Inhibitors.Molecules (Basel, Switzerland) · 2020Review
- Quorum Sensing Inhibitory and Antifouling Activities of New Bromotyrosine Metabolites from the Polynesian SpongeMarine drugs · 2020Article
- Plasmodial Kinase Inhibitors: License to Cure?Journal of medicinal chemistry · 2018Article
- Sponge chemical defenses are a possible mechanism for increasing sponge abundance on reefs in Zanzibar.PloS one · 2018Article
- Marine Sponges and Bacteria as Challenging Sources of Enzyme Inhibitors for Pharmacological Applications.Marine drugs · 2017Review
- Effects of Hangeshashinto on Growth of Oral Microorganisms.Evidence-based complementary and alternative medicine : eCAM · 2015Article
- Article
- Review
- Article
- Kinase inhibitors from marine sponges.Marine drugs · 2011Review
- The structural diversity and promise of antiparasitic marine invertebrate-derived small molecules.Current opinion in biotechnology · 2010Review
Corrections and comments
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Authors and funding
9 authors at 4 institutions in 4 countries.
Funding
No grant is acknowledged in the PubMed record.
Abstract
As part of our search for new antimalarial drugs in South Pacific marine sponges, we have looked for inhibitors of Pfnek-1, a specific protein kinase of Plasmodium falciparum. On the basis of promising activity in a preliminary screening, the ethanolic crude extract of a new species of Pseudoceratina collected in Vanuatu was selected for further investigation. A bioassay-guided fractionation led to the isolation of a derivative of homogentisic acid [methyl (2,4-dibromo-3,6-dihydroxyphenyl)acetate, 4a] which inhibited Pfnek-1 with an IC(50) around 1.8 muM. This product was moderately active in vitro against a FcB1 P. falciparum strain (IC(50) = 12 muM). From the same sponge, we isolated three known compounds [11,19-dideoxyfistularin-3 (1), 11-deoxyfistularin-3 (2) and dibromo-verongiaquinol (3)] which were inactive against Pfnek-1. Synthesis and biological evaluation of some derivatives of 4a are reported.
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