Evidence map›Paper›PMID 29655610›Full record

ArticleBioorganic & medicinal chemistry2018

Structure based drug design and in vitro metabolism study: Discovery of N-(4-methylthiophenyl)-N,2-dimethyl-cyclopenta[d]pyrimidine as a potent microtubule targeting agent.

Weiguo Xiang, Shruti Choudhary, Ernest Hamel, Susan L Mooberry, Aleem Gangjee

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2018. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.

0numbers the graph read from it
0cells of the map it votes in
4citing papers in PubMed
0.9field-weighted citation impact, top 30% 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

4 citing papers in PubMed, 10 citations in OpenAlex.

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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

5 authors at 3 institutions in 1 country.

Weiguo XiangDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States.
Shruti ChoudharyDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States.
Ernest HamelScreening Technologies Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, Frederick National Laboratory for Cancer Research, National Institutes of Health, Frederick, MD 21702, United States.
Susan L MooberryDepartment of Pharmacology, Cancer Therapy & Research Center, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, San Antonio, TX 78229, United States. Electronic address: mooberry@uthscsa.edu.
Aleem GangjeeDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States. Electronic address: gangjee@duq.edu.
Duquesne University · USFrederick National Laboratory for Cancer Research · USThe University of Texas Health Science Center at San Antonio · US

Funding

Water Soluble Antimitotics That Circumvent Rumor ResistanceR01CA142868 · NCI · DUQUESNE UNIVERSITY · PI GANGJEE, ALEEM, MOOBERRY, SUSAN L · 2011 to 2015
$1.5M
NCI NIH HHS R01 CA142868
6 · The paper itself

Abstract

We report a series of tubulin targeting agents, some of which demonstrate potent antiproliferative activities. These analogs were designed to optimize the antiproliferative activity of 1 by varying the heteroatom substituent at the 4'-position, the basicity of the 4-position amino moiety, and conformational restriction. The potential metabolites of the active compounds were also synthesized. Some compounds demonstrated single digit nanomolar IC

Indexed as

Antineoplastic AgentsBinding SitesCell Line, TumorDrug DesignDrug Resistance, NeoplasmHumansMicrosomes, LiverModels, MolecularMolecular ConformationMolecular Docking SimulationProtein BindingPyrimidinesStructure-Activity RelationshipTubulinTubulin ModulatorsAntineoplastic AgentsPyrimidinesTubulinTubulin ModulatorsCyclopenta[d]pyrimidineMetabolismMicrotubule targeting agent

Identifiers

PMID29655610
PMCPMC5967629
OpenAlexW2796260633

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.