ArticleAntimicrobial agents and chemotherapy1993
Structure-activity relationships and modes of action of 9-anilinoacridines against chloroquine-resistant Plasmodium falciparum in vitro.
Article in Antimicrobial agents and chemotherapy, 1993. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 18 papers.
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Who cites it
18 citing papers in PubMed, 70 citations in OpenAlex.
- N-(9-Acridinyl) Amino Acid Derivatives: Synthesis and In Vitro Evaluation of Anti-Pharmaceutics · 2025Article
- Pyronaridine: a review of its clinical pharmacology in the treatment of malaria.The Journal of antimicrobial chemotherapy · 2023Review
- A tale of topoisomerases and the knotty genetic material in the backdrop of Plasmodium biology.Bioscience reports · 2022Review
- The Antimalarial Drug Pyronaridine Inhibits Topoisomerase II in Breast Cancer Cells and Hinders Tumor ProgressionClinical cancer drugs · 2021Article
- Old drug repurposing for neglected disease: Pyronaridine as a promising candidate for the treatment of Echinococcus granulosus infections.EBioMedicine · 2020Article
- Pyronaridine exerts potent cytotoxicity on human breast and hematological cancer cells through induction of apoptosis.PloS one · 2018Article
- Review of pyronaridine anti-malarial properties and product characteristics.Malaria journal · 2012Article
- Global gene expression profiling of Plasmodium falciparum in response to the anti-malarial drug pyronaridine.Malaria journal · 2011Article
- Bioanalytical Screening of Riboflavin Antagonists for Targeted Drug Delivery - A Thermodynamic and Kinetic Study.ACS medicinal chemistry letters · 2011Article
- Synthesis and anti-intestinal nematode activity of variously substituted benzonaphthyridine derivatives.Molecules (Basel, Switzerland) · 2011Article
- Acridine and acridinones: old and new structures with antimalarial activity.The open medicinal chemistry journal · 2011Article
- DNA topoisomerases in apicomplexan parasites: promising targets for drug discovery.Proceedings. Biological sciences · 2010Review
- Absorption, distribution, excretion, and pharmacokinetics of 14C-pyronaridine tetraphosphate in male and female Sprague-Dawley rats.Journal of biomedicine & biotechnology · 2010Article
- Targeting of hematin by the antimalarial pyronaridine.Antimicrobial agents and chemotherapy · 2006Article
- Antimalarial 9-anilinoacridine compounds directed at hematin.Antimicrobial agents and chemotherapy · 2003Article
- Effect of structure on antibiotic action of new 9-(ethylthio)acridines.Folia microbiologica · 2002Article
- In vivo monitoring of intracellular ATP levels in Leishmania donovani promastigotes as a rapid method to screen drugs targeting bioenergetic metabolism.Antimicrobial agents and chemotherapy · 2001Article
- The gene encoding topoisomerase II from Plasmodium falciparum.Nucleic acids research · 1994Article
Corrections and comments
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Authors and funding
6 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
An in vitro investigation of the structure-activity profiles for a range of 9-anilinoacridines on drug-resistant Plasmodium falciparum is reported. C-3, 6-diamino substitution, low lipophilicity, and high pKa values substantially increased the activities of the 9-anilinoacridines tested. There appeared to be no correlation between DNA binding and antimalarial activity. 3,6-Diamino-1'-amino-9-anilinoacridine (compound 13) was the most active compound tested; it had a 50% inhibitory concentration of 25 nM. In vitro mammalian cell growth assays showed compound 13 to be one of the least cytotoxic 9-anilinoacridines (50% inhibitory concentration, 15 microM). Both compound 13 and the antimalarial drug pyronaridine inhibited the decatenation activity of P. falciparum DNA topoisomerase II at concentrations of 10 and 11 microM, respectively.
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