Evidence map›Paper›PMID 30833159›Full record

ArticleBioorganic & medicinal chemistry2019

Lead optimization of selective tubulin inhibitors as anti-trypanosomal agents.

Anran Zhao, Yaxin Li, Cody M Orahoske, Brittny Schnur, Abboud Sabbagh, Wenjing Zhang, Bibo Li, Bin Su

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Bioorganic & medicinal chemistry, 2019. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Article
  2. Triflamides and Triflimides: Synthesis and Applications.Molecules (Basel, Switzerland) · 2022
    Review
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

8 authors.

Anran ZhaoDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Yaxin LiDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, 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 Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Brittny SchnurDepartment of Biology, Geo. & Env. Sciences, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Abboud SabbaghDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA.
Wenjing ZhangDepartment of Chemistry, Center for Gene Regulation in Health and Disease, College of Sciences and Health Professions, 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 Sciences and Health Professions, 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 Sciences and Health Professions, Cleveland State University, 2121 Euclid Ave., Cleveland, OH 44115, USA. Electronic address: b.su@csuohio.edu.

Funding

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 R15 AI103889NIH HHS S10 OD025252
6 · The paper itself

Abstract

Previously synthesized tubulin inhibitors showed promising in vitro selectivity and activity against Human African Trypanosomiasis. Current aim is to improve the ligand efficiency and reduce overall hydrophobicity of the compounds, by lead optimization. Via combinatorial chemistry, 60 new analogs were synthesized. For biological assay Trypanosoma brucei brucei Lister 427 cell line were used as the parasite model and for the host model human embryonic kidney cell line HEK-293 and mouse macrophage cell line RAW 264.7 were used to test efficacy. Of the newly synthesized compounds 5, 39, 40, and 57 exhibited IC

Indexed as

AnimalsDrug DesignDrug DiscoveryHEK293 CellsHumansMiceRAW 264.7 CellsTrypanocidal AgentsTrypanosoma brucei bruceiTrypanosomiasis, AfricanTubulin ModulatorsTrypanocidal AgentsTubulin ModulatorsDrug developmentLead optimizationTrypanosomiasisTubulin inhibitor

Identifiers

PMID30833159
PMCPMC6531046

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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.