Evidence map›Paper›PMID 27156776›Full record

ArticleBioorganic & medicinal chemistry letters2016

In vitro evaluation of imidazo[4,5-c]quinolin-2-ones as gametocytocidal antimalarial agents.

Paresma R Patel, Wei Sun, Myunghoon Kim, Xiuli Huang, Philip E Sanderson, Takeshi Q Tanaka, John C McKew, Anton Simeonov, Kim C Williamson, Wei Zheng and 1 more

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 3 papers.

0numbers the graph read from it
0cells of the map it votes in
3citing papers in PubMed
–field-weighted citation impact
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

3 citing papers in PubMed.

  1. Review
  2. Article
  3. 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

11 authors.

Paresma R PatelNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
Wei SunNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
Myunghoon KimNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
Xiuli HuangNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
Philip E SandersonNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
Takeshi Q TanakaDepartment of Biology, Loyola University Chicago, Chicago, IL 60660, United States.
John C McKewNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
Anton SimeonovNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
Kim C WilliamsonDepartment of Biology, Loyola University Chicago, Chicago, IL 60660, United States.
Wei ZhengNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States.
Wenwei HuangNational Center for Advancing Translational Sciences, National Institutes of Health, Bethesda, MD 20892, United States. Electronic address: huangwe@mail.nih.gov.

Funding

Drug Repurposing Screening for Rare and Neglected DiseasesZIATR000018 · NCATS · NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES · PI ZHENG, WEI · 2015 to 2025
$24.6M
Development of Malaria Transmission-Blocking DrugsZIATR000013 · NCATS · NATIONAL CENTER FOR ADVANCING TRANSLATIONAL SCIENCES · PI HUANG, WENWEI · 2015 to 2025
$19.3M
Advancing gametocytocidal agents as drugs against P. falciparumR01AI114761 · NIAID · LOYOLA UNIVERSITY OF CHICAGO · PI WILLIAMSON, KIM C · 2015 to 2019
$1.9M
Targeting P. falciparum gametocytes for drug developmentR21AI101396 · NIAID · LOYOLA UNIVERSITY OF CHICAGO · PI WILLIAMSON, KIM C · 2012 to 2013
$374k
Intramural NIH HHS Z99 TR999999NIAID NIH HHS R01 AI114761NIAID NIH HHS R21 AI101396
6 · The paper itself

Abstract

Novel imidazo[4,5-c]quinolin-2-ones were synthesized and evaluated in asexual blood stage and late stage gametocyte assays of Plasmodium falciparum, a major causative agent of malaria. The design of these compounds is based on a recently identified lead compound from a high throughput screen. A concise synthesis was developed that allowed for generation of analogues with substitution around both the quinoline and imidazolidinone rings. Through structure-activity relationship studies, a number of potent compounds were identified that possessed excellent antimalarial activity against both the asexual and sexual stages with minimal cytotoxicity in mammalian cells. This is the first Letter describing SAR and gametocytocidal activity of imidazo[4,5-c]quinolin-2-ones, a new lead series for malaria treatment and prevention.

Indexed as

AntimalarialsCell SurvivalDose-Response Relationship, DrugHep G2 CellsHigh-Throughput Screening AssaysHumansImidazolesMalariaMolecular StructureParasitic Sensitivity TestsPlasmodium falciparumQuinolonesStructure-Activity RelationshipAntimalarialsimidazo(4,5-c)quinolin-2-oneImidazolesQuinolonesAntimalarialGametocytesGametocytocidalImidazo[4,5-c]quinolin-2-onePlasmodium falciparum

Identifiers

PMID27156776
PMCPMC4887403

What OpenQuestion holds

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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.