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Simple and Inexpensive Fluorescence-Based Technique for High-Throughput Antimalarial Drug Screening
- M. Smilkstein, N. Sriwilaijaroen, J. X. Kelly, P. Wilairat, M. Riscoe
- Biology, MedicineAntimicrobial Agents and Chemotherapy
- 1 May 2004
A side-by-side comparison of this new fluorescence assay and a standard radioisotopic method suggest that it may be an ideal method for high-throughput antimalarial drug screening.
Discovery of dual function acridones as a new antimalarial chemotype
This innovative acridone design merges intrinsic potency and resistance-counteracting functions in one molecule, and represents a new strategy to expand, enhance and sustain effective antimalarial drug combinations.
A chloroquine-like molecule designed to reverse resistance in Plasmodium falciparum.
- S. Burgess, A. Selzer, J. X. Kelly, M. Smilkstein, M. Riscoe, D. Peyton
- ChemistryJournal of medicinal chemistry
- 7 September 2006
A preliminary study in mice demonstrated oral efficacy against P. chabaudi and the absence of obvious toxicity, and the RCQ approach appears to be feasible.
Evaluation and lead optimization of anti-malarial acridones.
Xanthones as antimalarial agents: discovery, mode of action, and optimization.
It is revealed how these compounds target the Plasmodium parasite's most vulnerable feature--the digestive vacuole.
Antimalarial activity of natural and synthetic prodiginines.
- Kancharla Papireddy, M. Smilkstein, K. Reynolds
- Chemistry, BiologyJournal of medicinal chemistry
- 8 July 2011
The in vitro antimalarial activity of four natural and three sets of synthetic prodiginines against Plasmodium falciparum was described and each analogue reduced parasitemia by more than 90% after 25 (mg/kg)/day dosing and in some cases provided a cure.
Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds.
An investigation into the structure-activity relationship of the RCQ structures results in an orally active molecule with good in vitro and in vivo antimalarial activity, and evidence of the mode of action is presented, indicating that the RC Q molecules inhibit hemozoin formation in the parasite's digestive vacuole in a manner similar to that of chloroquine.
A drug-selected Plasmodium falciparum lacking the need for conventional electron transport.
Design, Synthesis, and Evaluation of 10-N-Substituted Acridones as Novel Chemosensitizers in Plasmodium falciparum
- J. X. Kelly, M. Smilkstein, M. Riscoe
- ChemistryAntimicrobial Agents and Chemotherapy
- 10 September 2007
The combined results indicate that 10-N-substituted acridones present novel pharmacophores for the development of chemosensitizers against P. falciparum.