Evidence map›Paper›PMID 32390431›Full record

ArticleJournal of medicinal chemistry2020

Lead Optimization of Second-Generation Acridones as Broad-Spectrum Antimalarials.

Papireddy Kancharla, Rozalia A Dodean, Yuexin Li, Sovitj Pou, Brandon Pybus, Victor Melendez, Lisa Read, Charles E Bane, Brian Vesely, Mara Kreishman-Deitrick and 32 more

Open access · greenAbstract read
In one paragraph

Article in Journal of medicinal chemistry, 2020. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.

0numbers the graph read from it
0cells of the map it votes in
14citing papers in PubMed
1.6field-weighted citation impact, top 15% of its field
1 · What the graph read from it

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.

2 · The registry

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.

Neither the registry nor the abstract names a trial number. If this is a trial report, that itself is worth knowing.

3 · Its place in the literature

Who cites it

14 citing papers in PubMed, 16 citations in OpenAlex.

  1. Article
  2. Evaluating acridones as novel therapeutics for human babesiosis.Antimicrobial agents and chemotherapy · 2026
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  3. Identification of an Orally Efficacious Imidazo[4,5-Journal of medicinal chemistry · 2026
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  5. Targeting Mitochondrial Function inInternational journal of molecular sciences · 2025
    Review
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  9. Structure-activity relationships ofExpert opinion on drug discovery · 2022
    Article
  10. Antimalarial Natural Products.Progress in the chemistry of organic natural products · 2022
    Article
  11. Article
  12. Acridones Are Highly Potent Inhibitors ofACS infectious diseases · 2021
    Article
  13. Total Synthesis and Antimalarial Activity of 2-(Journal of medicinal chemistry · 2021
    Article
  14. Article
4 · The record

Corrections and comments

PubMed lists nothing against this paper. Absence here is not a guarantee, only a check that was made.

5 · Who and what money

Authors and funding

42 authors at 7 institutions in 2 countries.

Papireddy KancharlaDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0002-6381-1236
Rozalia A DodeanDepartment of Veterans Affairs Medical Center, Portland, Oregon 97239, United States.ORCID 0000-0001-5002-4607
Yuexin LiDepartment of Veterans Affairs Medical Center, Portland, Oregon 97239, United States.
Sovitj PouDepartment of Veterans Affairs Medical Center, Portland, Oregon 97239, United States.
Brandon PybusDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Victor MelendezDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Lisa ReadDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Charles E BaneDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Brian VeselyDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Mara Kreishman-DeitrickDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Chad BlackDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Qigui LiDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Richard J SciottiDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Raul OlmedaDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Thu-Lan LuongDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Heather GaonaDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Brittney PotterDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Jason SousaDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Sean MarcsisinDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Diana CaridhaDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Lisa XieDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Chau VuongDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Qiang ZengDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Jing ZhangDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Ping ZhangDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Hsiuling LinDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Kirk ButlerDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Norma RoncalDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Lacy Gaynor-OhnstadDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Susan E LeedDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Christina NolanDivision of Experimental Therapeutics, Walter Reed Army Institute of Research, Silver Spring, Maryland 20910, United States.
Frida G CejaDepartment of Natural Sciences and Mathematics, Dominican University of California, San Rafael, California 94901, United States.
Stephanie A RasmussenDepartment of Natural Sciences and Mathematics, Dominican University of California, San Rafael, California 94901, United States.
Patrick K TumwebazeInfectious Diseases Research Collaboration, Kampala, Uganda.
Philip J RosenthalDepartment of Medicine, University of California, San Francisco, San Francisco, California 94143, United States.
Jianbing MuLaboratory of Malaria and Vector Research, National Institute of Allergy and Infectious Diseases, National Institutes of Health, Rockville, Maryland 20852, United States.ORCID 0000-0001-6012-8389
Brett R BaylesDepartment of Natural Sciences and Mathematics, Dominican University of California, San Rafael, California 94901, United States.
Roland A CooperDepartment of Natural Sciences and Mathematics, Dominican University of California, San Rafael, California 94901, United States.
Kevin A ReynoldsDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0003-0270-9809
Martin J SmilksteinDepartment of Veterans Affairs Medical Center, Portland, Oregon 97239, United States.
Michael K RiscoeDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.
Jane X KellyDepartment of Chemistry, Portland State University, Portland, Oregon 97201, United States.ORCID 0000-0001-8871-0207
Walter Reed Army Institute of Research · USDominican University of California · USPortland State University · USPortland VA Medical Center · USInfectious Diseases Research Collaboration · UGNational Institutes of Health · USUniversity of California, San Francisco · US

Funding

Novel Broad-spectrum AntimalarialsR01AI093784 · NIAID · PORTLAND STATE UNIVERSITY · PI KELLY, JANE X, KREISHMAN-DEITRICK, MARA · 2012 to 2016
$3.5M
NIAID NIH HHS R01 AI093784
6 · The paper itself

Abstract

The global impact of malaria remains staggering despite extensive efforts to eradicate the disease. With increasing drug resistance and the absence of a clinically available vaccine, there is an urgent need for novel, affordable, and safe drugs for prevention and treatment of malaria. Previously, we described a novel antimalarial acridone chemotype that is potent against both blood-stage and liver-stage malaria parasites. Here, we describe an optimization process that has produced a second-generation acridone series with significant improvements in efficacy, metabolic stability, pharmacokinetics, and safety profiles. These findings highlight the therapeutic potential of dual-stage targeting acridones as novel drug candidates for further preclinical development.

Indexed as

AcridonesAdministration, OralAnimalsAntimalarialsCell SurvivalDisease Models, AnimalFemaleHalf-LifeHep G2 CellsHumansLife Cycle StagesMalariaMaleMiceMice, Inbred C57BLPlasmodium falciparumAcridonesAntimalarials

Identifiers

PMID32390431
PMCPMC7354843
OpenAlexW3022197165

What OpenQuestion holds

Textmetadata
LicenceTDM
Read underepoch 390

Registered trials

None linked

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.