Evidence map›Paper›PMID 38762979›Full record

ArticleBioorganic & medicinal chemistry2024

Synthesis and biological evaluation of orally active anti-Trypanosoma agents.

Fatma M Salem, William R Martin, Xiaotong Zhao, S K Adbus Sayeed, Sabreena Ighneim, McKenna Greene, Eman Mohamed, Cody M Orahoske, Wenjing Zhang, Bibo Li and 1 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing 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

1 citing paper in PubMed.

  1. Veterinary world · 2025
    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.

Fatma M SalemDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
William R MartinDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA; Genomic Medicine Institute, Cleveland Clinic Genome Center, Lerner Research Institute, Cleveland Clinic, Cleveland, OH 44195, USA.
Xiaotong ZhaoDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
S K Adbus SayeedDepartment of Biology, Geo. & Env. Sciences, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Sabreena IghneimDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
McKenna GreeneDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Eman MohamedDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Cody M OrahoskeDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Wenjing ZhangDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Bibo LiDepartment of Biology, Geo. & Env. Sciences, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA. Electronic address: b.li37@csuohio.edu.
Bin SuDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Arts and Sciences, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA. Electronic address: b.su@csuohio.edu.

Funding

Mechanisms of RAP1 functions in monoallelic VSG expression in Trypanosoma bruceiR01AI066095 · NIAID · CLEVELAND STATE UNIVERSITY · PI LI, BIBO · 2007 to 2020
$5.2M
Essential functions of Trypanosoma brucei RAP1R01AI179972 · NIAID · CLEVELAND STATE UNIVERSITY · PI Bibo Li · 2024 to 2026
$1.3M
Selective tubulin inhibitors with improved cell update for kinetoplastid infectionsR15AI103889 · NIAID · CLEVELAND STATE UNIVERSITY · PI SU, BIN · 2013 to 2016
$873k
A Digital Laser Scanner Biomolecular Imaging System: Amersham Typhoon 5S10OD025252 · OD · CLEVELAND STATE UNIVERSITY · PI LI, BIBO · 2018 to 2018
$163k
NIAID NIH HHS R01 AI066095NIAID NIH HHS R01 AI179972NIAID NIH HHS R15 AI103889NIH HHS S10 OD025252
6 · The paper itself

Abstract

In previous studies, we developed anti-trypanosome tubulin inhibitors with promising in vitro selectivity and activity against Human African Trypanosomiasis (HAT). However, for such agents, oral activity is crucial. This study focused on further optimizing these compounds to enhance their ligand efficiency, aiming to reduce bulkiness and hydrophobicity, which should improve solubility and, consequently, oral bioavailability. Using Trypanosoma brucei brucei cells as the parasite model and human normal kidney cells and mouse macrophage cells as the host model, we evaluated 30 new analogs synthesized through combinatorial chemistry. These analogs have fewer aromatic moieties and lower molecular weights than their predecessors. Several new analogs demonstrated IC

Indexed as

Trypanocidal AgentsTrypanosoma brucei bruceiAdministration, OralAnimalsCell ProliferationDose-Response Relationship, DrugHumansMiceMolecular Docking SimulationMolecular StructureParasitic Sensitivity TestsStructure-Activity RelationshipTrypanosomiasis, AfricanTubulinTubulin ModulatorsTrypanocidal AgentsTubulinTubulin ModulatorsDrug developmentLead optimizationLigand efficiencyTrypanosomiasisTubulin inhibitor

Identifiers

PMID38762979
PMCPMC12798742

What OpenQuestion holds

Textmetadata
LicenceCC BY-NC-ND
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.