Evidence map›Paper›PMID 28610978›Full record

ArticleBioorganic & medicinal chemistry letters2017

Design, synthesis, and structure-activity relationships of pyrimido[4,5-b]indole-4-amines as microtubule depolymerizing agents that are effective against multidrug resistant cells.

Ravi Kumar Vyas Devambatla, Wei Li, Nilesh Zaware, Shruti Choudhary, Ernest Hamel, Susan L Mooberry, Aleem Gangjee

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2017. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing papers in PubMed
0.7field-weighted citation impact, top 33% 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

5 citing papers in PubMed, 14 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

7 authors at 3 institutions in 1 country.

Ravi Kumar Vyas DevambatlaDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States.
Wei LiDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States.
Nilesh ZawareDivision 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

To identify the structural features of 9H-pyrimido[4,5-b]indoles as microtubule depolymerizers, pyrimido[4,5-b]indoles 2-8 with varied substituents at the 2-, 4- and 5-positions were designed and synthesized. Nucleophilic displacement of 2,5-substituted-4-chloro-pyrimido[4,5-b]indoles with appropriate arylamines was the final step employed in the synthesis of target compounds 2-8. Compounds 2 and 6 had two-digit nanomolar potency (IC

Indexed as

Drug Resistance, NeoplasmAminationAntineoplastic AgentsCell Line, TumorDrug Resistance, MultipleHumansIndolesMicrotubulesMolecular Docking SimulationNeoplasmsPyrimidinesStructure-Activity RelationshipTubulinTubulin ModulatorsAntineoplastic AgentsIndolesPyrimidinesTubulinTubulin ModulatorsConformational restrictionMicrotubule depolymerizing agentsMicrotubulesMultidrug resistancePyrimido[4,5-b]indoles

Identifiers

PMID28610978
PMCPMC5603926
OpenAlexW2617964299

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.