ArticleJournal of medicinal chemistry2010
Synthesis, structure-activity relationship, and mode-of-action studies of antimalarial reversed chloroquine compounds.
Article in Journal of medicinal chemistry, 2010. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 23 papers.
What it found
Each row is one number read from the abstract, on the scale the paper reported it, with its interval. Left of the dashed line favours the treatment, right favours the comparator. Under each row is the sentence it came from. New to these charts? A ten-minute tutorial.
The abstract states no effect estimate the extractor could read, or names no intervention and outcome on the map, so this paper lights no cell and moves no belief. It is still indexed, cited and linked below.
The trial behind it
Trials whose registry record cites this paper, or whose number appears in the abstract. A trial that started after this paper was published is citing it as background, not reporting it.
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Who cites it
23 citing papers in PubMed, 97 citations in OpenAlex.
- Quinoline derivatives' biological interest for anti-malarial and anti-cancer activities: an overview.RSC advances · 2025Review
- Exploring Quinoline Derivatives: Their Antimalarial Efficacy and Structural Features.Medicinal chemistry (Shariqah (United Arab Emirates)) · 2025Review
- Biological evaluation of novel side chain containing CQTrICh-analogs as antimalarials and their development asHeliyon · 2024Article
- Quinoline as a Privileged Structure: A Recent Update on Synthesis and Biological Activities.Current topics in medicinal chemistry · 2024Review
- Is structural hybridization invoking new dimensions for antimalarial drug discovery research?RSC medicinal chemistry · 2023Review
- Synthesis and Antileishmanial Evaluation of Arylimidamide-Azole Hybrids Containing a Phenoxyalkyl Linker.ACS infectious diseases · 2021Article
- Article
- Correlation between anti-malarial and anti-haemozoin activities of anti-malarial compounds.Malaria journal · 2020Article
- Unsymmetrical Bisquinolines with High Potency againstMolecules (Basel, Switzerland) · 2020Article
- The past, present and future of anti-malarial medicines.Malaria journal · 2019Review
- Synthesis, Biological Evaluation, and Molecular Modeling Studies of Chiral Chloroquine Analogues as Antimalarial Agents.Antimicrobial agents and chemotherapy · 2018Article
- Simplified Reversed Chloroquines To Overcome Malaria Resistance to Quinoline-Based Drugs.Antimicrobial agents and chemotherapy · 2017Article
- Introducing New Antimalarial Analogues of Chloroquine and Amodiaquine: A Narrative Review.Iranian journal of medical sciences · 2017Review
- Evaluation of Novel α-(Acyloxy)-α-(Quinolin-4-yl) Acetamides as Antiplasmodial Agents.Iranian journal of pharmaceutical research : IJPR · 2017Article
- Overcoming Chloroquine Resistance in Malaria: Design, Synthesis, and Structure-Activity Relationships of Novel Hybrid Compounds.Antimicrobial agents and chemotherapy · 2016Article
- Contrasting ex vivo efficacies of "reversed chloroquine" compounds in chloroquine-resistant Plasmodium falciparum and P. vivax isolates.Antimicrobial agents and chemotherapy · 2015Article
- Second generation steroidal 4-aminoquinolines are potent, dual-target inhibitors of the botulinum neurotoxin serotype A metalloprotease and P. falciparum malaria.Journal of medicinal chemistry · 2014Article
- Dual-functioning antimalarials that inhibit the chloroquine-resistance transporter.Future microbiology · 2013Review
- Know your enemy: understanding the role of PfCRT in drug resistance could lead to new antimalarial tactics.Cellular and molecular life sciences : CMLS · 2012Review
- Reversed chloroquine molecules as a strategy to overcome resistance in malaria.Current topics in medicinal chemistry · 2012Review
Corrections and comments
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Authors and funding
7 authors at 4 institutions in 2 countries.
Funding
Abstract
We have previously shown that a "reversed chloroquine (RCQ)" molecule, composed of a chloroquine-like moiety and a resistance reversal-like moiety, can overcome chloroquine resistance in P. falciparum ( Burgess , S. J. ; Selzer , A. ; Kelly , J. X. ; Smilkstein , M. J. ; Riscoe , M. K. ; Peyton , D. H. J. Med. Chem. 2006 , 49 , 5623 . Andrews , S. ; Burgess , S. J. ; Skaalrud , D. ; Kelly , J. X. ; Peyton , D. H. J. Med. Chem. 2010 , 53 , 916 ). Here, we present an investigation into the structure-activity relationship of the RCQ structures, resulting in an orally active molecule with good in vitro and in vivo antimalarial activity. We also present evidence of the mode of action, indicating that the RCQ molecules inhibit hemozoin formation in the parasite's digestive vacuole in a manner similar to that of chloroquine.
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Registered trials
Read under generation 80e0d062 · epoch 390. Bibliography from PubMed, PubMed Central and OpenAlex; grants from NIH RePORTER; trial links from ClinicalTrials.gov; estimates, votes and beliefs from the OpenQuestion graph.