Evidence map›Paper›PMID 36608774›Full record

ArticleBioorganic & medicinal chemistry letters2023

Structure-activity relationship of dibenzylideneacetone analogs against the neglected disease pathogen, Trypanosoma brucei.

Karol R Francisco, Ludovica Monti, Wenqian Yang, Hayoung Park, Lawrence J Liu, Kaitlyn Watkins, Dilini K Amarasinghe, Marianna Nalli, Carlos Roberto Polaquini, Luis O Regasini and 4 more

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2023. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 13 papers.

0numbers the graph read from it
0cells of the map it votes in
13citing 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

13 citing papers in PubMed.

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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

14 authors.

Karol R FranciscoCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA. Electronic address: krfranci@ucsd.edu.
Ludovica MontiCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Wenqian YangCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Hayoung ParkCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Lawrence J LiuCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Kaitlyn WatkinsCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Dilini K AmarasingheCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.
Marianna NalliLaboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, 00185 Rome, Italy.
Carlos Roberto PolaquiniInstitute of Biosciences, Humanities and Exact Sciences, São Paulo State University, São José do Rio Preto, SP 15054-000, Brazil.
Luis O RegasiniInstitute of Biosciences, Humanities and Exact Sciences, São Paulo State University, São José do Rio Preto, SP 15054-000, Brazil.
Antônio Eduardo Miller CrottiFaculty of Philosophy, Sciences, and Letters of Ribeirão Preto, University of São Paulo, Ribeirão Preto, SP 14040-900, Brazil.
Romano SilvestriLaboratory Affiliated with the Institute Pasteur Italy - Cenci Bolognetti Foundation, Department of Drug Chemistry and Technologies, Sapienza University of Rome, 00185 Rome, Italy.
Lizandra Guidi MagalhãesResearch Group on Natural Products, Center for Research in Sciences and Technology, University of Franca, Franca, SP 14404-600, Brazil.
Conor R CaffreyCenter for Discovery and Innovation in Parasitic Diseases, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of California, San Diego, La Jolla, CA 92093, USA.

Funding

RESEARCH IN INFECTIOUS DISEASEST32AI007036 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI NIZET, VICTOR · 1985 to 2025
$9.2M
Brain Penetrant Microtubule-Stabilizers to Treat CNS-invasive Parasitic DiseasesR21AI141210 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI BALLATORE, CARLO, CAFFREY, CONOR · 2019 to 2020
$441k
The catalytic core of the proteasome as a drug target to treat Human African TrypanosomiasisR21AI171824 · NIAID · UNIVERSITY OF CALIFORNIA, SAN DIEGO · PI CAFFREY, CONOR, O'DONOGHUE, ANTHONY JOHN · 2022 to 2023
$435k
NIAID NIH HHS R21 AI141210NIAID NIH HHS R21 AI171824NIAID NIH HHS T32 AI007036
6 · The paper itself

Abstract

Trypanosoma brucei is a protozoan parasite that causes Human African Trypanosomiasis (HAT), a neglected tropical disease (NTD) that is endemic in 36 countries in sub-Saharan Africa. Only a handful drugs are available for treatment, and these have limitations, including toxicity and drug resistance. Using the natural product, curcumin, as a starting point, several curcuminoids and related analogs were evaluated against bloodstream forms of T. b. brucei. A particular subset of dibenzylideneacetone (DBA) compounds exhibited potent in vitro antitrypanosomal activity with sub-micromolar EC

Indexed as

Trypanocidal AgentsTrypanosoma brucei bruceiTrypanosomiasis, AfricanAnimalsHEK293 CellsHumansNeglected DiseasesStructure-Activity RelationshipTrypanocidal AgentsAntiparasitic activityCurcuminoidCytotoxicityDibenzylideneacetoneTrypanosoma brucei

Identifiers

PMID36608774
PMCPMC10072319

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.