Evidence map›Paper›PMID 30297118›Full record

ArticleBioorganic & medicinal chemistry2018

Sterically induced conformational restriction: Discovery and preclinical evaluation of novel pyrrolo[3,2-d]pyrimidines as microtubule targeting agents.

Roheeth Kumar Pavana, Khushbu Shah, Taylor Gentile, Nicholas F Dybdal-Hargreaves, April L Risinger, Susan L Mooberry, Ernest Hamel, Aleem Gangjee

Open access · greenAbstract read
PubMed Full text at PMC Publisher
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 1 paper.

0numbers the graph read from it
0cells of the map it votes in
1citing papers in PubMed
0.3field-weighted citation impact, top 42% 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

1 citing paper in PubMed, 6 citations in OpenAlex.

  1. 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

8 authors at 3 institutions in 1 country.

Roheeth Kumar PavanaDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, Pittsburgh, PA 15282, United States.
Khushbu ShahDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, Pittsburgh, PA 15282, United States.
Taylor GentileDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, Pittsburgh, PA 15282, United States.
Nicholas F Dybdal-HargreavesDepartment of Pharmacology, Mays Cancer Center, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, San Antonio, TX 78229, United States.
April L RisingerDepartment of Pharmacology, Mays Cancer Center, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, San Antonio, TX 78229, United States.
Susan L MooberryDepartment of Pharmacology, Mays Cancer Center, University of Texas Health Science Center at San Antonio, 7703 Floyd Curl Drive, San Antonio, TX 78229, United States.
Ernest HamelScreening Technologies Branch, Developmental Therapeutics Program, Division of Cancer Treatment and Diagnosis, National Cancer Institute at Frederick, National Institutes of Health, Frederick, MD 21702, United States.
Aleem GangjeeDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, Pittsburgh, PA 15282, United States. Electronic address: gangjee@duq.edu.
Duquesne University · USThe University of Texas Health Science Center at San Antonio · USNational Cancer Institute · US

Funding

Institutional Research Training GrantT32DE014318 · NIDCR · UNIVERSITY OF TEXAS HLTH SCIENCE CENTER · PI Kenneth M Hargreaves · 2002 to 2026
$12.1M
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 CA142868NIDCR NIH HHS T32 DE014318
6 · The paper itself

Abstract

The discovery, synthesis and biological evaluations of a series of nine N5-substituted-pyrrolo[3,2-d]pyrimidin-4-amines are reported. Novel compounds with microtubule depolymerizing activity were identified. Some of these compounds also circumvent clinically relevant drug resistance mechanisms (expression of P-glycoprotein and βIII tubulin). Compounds 4, 5, and 8-13 were one to two-digit nanomolar (IC

Indexed as

AnimalsAntineoplastic AgentsATP Binding Cassette Transporter, Subfamily B, Member 1Cell Line, TumorDrug Screening Assays, AntitumorFemaleHumansMice, NudeMicrotubulesMolecular Docking SimulationNeoplasmsPyrimidinesPyrrolesStereoisomerismTubulinTubulin ModulatorsAntineoplastic AgentsATP Binding Cassette Transporter, Subfamily B, Member 1PyrimidinesPyrrolesPyrrolo(2,3-d)pyrimidineTubulinTubulin ModulatorsMicrotubule depolymerizersMicrotubule targeting agentsP-glycoproteinPreclinical agentsPyrrolo[3, 2-d]pyrimidinesβIII tubulin

Identifiers

PMID30297118
PMCPMC6252143
OpenAlexW2893875505

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.