Evidence map›Paper›PMID 26641132›Full record

ArticleJournal of medicinal chemistry2016

Novel Microtubule-Targeting 7-Deazahypoxanthines Derived from Marine Alkaloid Rigidins with Potent in Vitro and in Vivo Anticancer Activities.

Derek C Medellin, Qiong Zhou, Robert Scott, R Matthew Hill, Sarah K Frail, Ramesh Dasari, Steven J Ontiveros, Stephen C Pelly, Willem A L van Otterlo, Tania Betancourt and 7 more

Abstract read
In one paragraph

Article in Journal of medicinal chemistry, 2016. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 8 papers.

0numbers the graph read from it
0cells of the map it votes in
8citing 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

8 citing papers in PubMed.

  1. Review
  2. Article
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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

17 authors.

Derek C MedellinDepartment of Chemistry and Biochemistry, Texas State University , San Marcos, Texas 78666, United States.
Qiong ZhouDepartment of Pharmaceutical Sciences, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus , Aurora, Colorado 80045, United States.
Robert ScottDepartment of Chemistry and Biochemistry, Texas State University , San Marcos, Texas 78666, United States.
R Matthew HillDepartment of Chemistry and Biochemistry, Texas State University , San Marcos, Texas 78666, United States.
Sarah K FrailDepartments of Chemistry and Biology, New Mexico Tech , Socorro, New Mexico 87801, United States.
Ramesh DasariDepartment of Chemistry and Biochemistry, Texas State University , San Marcos, Texas 78666, United States.
Steven J OntiverosDepartment of Biology, New Mexico State University , Las Cruces, New Mexico 88003, United States.
Stephen C PellyDepartment of Chemistry and Polymer Science, Stellenbosch University , Stellenbosch, Western Cape, South Africa.
Willem A L van OtterloDepartment of Chemistry and Polymer Science, Stellenbosch University , Stellenbosch, Western Cape, South Africa.
Tania BetancourtDepartment of Chemistry and Biochemistry, Texas State University , San Marcos, Texas 78666, United States.
Charles B ShusterDepartment of Biology, New Mexico State University , Las Cruces, New Mexico 88003, United States.
Ernest HamelScreening Technologies Branch, Developmental Therapeutics Program, National Cancer Institute, Frederick National Laboratory of Cancer Research, National Institutes of Health, Frederick, Maryland 21702, United States.
Ruoli BaiScreening Technologies Branch, Developmental Therapeutics Program, National Cancer Institute, Frederick National Laboratory of Cancer Research, National Institutes of Health, Frederick, Maryland 21702, United States.
Daniel V LaBarberaDepartment of Pharmaceutical Sciences, Skaggs School of Pharmacy and Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus , Aurora, Colorado 80045, United States.
Snezna RogeljDepartments of Chemistry and Biology, New Mexico Tech , Socorro, New Mexico 87801, United States.
Liliya V FrolovaDepartments of Chemistry and Biology, New Mexico Tech , Socorro, New Mexico 87801, United States.
Alexander KornienkoDepartment of Chemistry and Biochemistry, Texas State University , San Marcos, Texas 78666, United States.

Funding

NM-INBRE Sequencing and Bioinformatics CoreP20GM103451 · NIGMS · NEW MEXICO STATE UNIVERSITY LAS CRUCES · PI Charlotte C. Gard · 2012 to 2026
$61.2M
Mob1 Localization and Function During MitosisSC1HD063917 · NICHD · NEW MEXICO STATE UNIVERSITY LAS CRUCES · PI SHUSTER, CHARLES BRADLEY · 2009 to 2012
$975k
Mode of Action of the Amaryllidaceae Alkaloid Lycorine-Promising Anticancer AgentR15CA186046 · NCI · TEXAS STATE UNIVERSITY · PI KORNIENKO, ALEXANDER · 2014 to 2014
$476k
NCI NIH HHS CA186046-01A1NCI NIH HHS R15 CA186046NICHD NIH HHS 5SC1HD063917NICHD NIH HHS SC1 HD063917NIGMS NIH HHS P20 GM103451NIGMS NIH HHS P20GM103451
6 · The paper itself

Abstract

Docking studies of tubulin-targeting C2-substituted 7-deazahypoxanthine analogues of marine alkaloid rigidins led to the design and synthesis of compounds containing linear C2-substituents. The C2-alkynyl analogue was found to have double- to single-digit nanomolar antiproliferative IC50 values and showed statistically significant tumor size reduction in a colon cancer mouse model at nontoxic concentrations. These results provide impetus and further guidance for the development of these rigidin analogues as anticancer agents.

Indexed as

AnimalsAntineoplastic AgentsCell Line, TumorCell ProliferationColchicineColonic NeoplasmsDrug DesignDrug Screening Assays, AntitumorFemaleHumansMarine ToxinsMiceMice, NudeModels, MolecularMolecular Docking SimulationStructure-Activity RelationshipAntineoplastic AgentsColchicineMarine ToxinsTubulinTubulin ModulatorsXanthines

Identifiers

PMID26641132
PMCPMC4950951

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.