Evidence map›Paper›PMID 22739090›Full record

ArticleBioorganic & medicinal chemistry2012

Novel tricyclic indeno[2,1-d]pyrimidines with dual antiangiogenic and cytotoxic activities as potent antitumor agents.

Aleem Gangjee, Ying Zhao, Michael A Ihnat, Jessica E Thorpe, Lora C Bailey-Downs, Roy L Kisliuk

Open access · greenAbstract read
In one paragraph

Article in Bioorganic & medicinal chemistry, 2012. 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
0.6field-weighted citation impact, top 32% 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, 9 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

6 authors at 3 institutions in 1 country.

Aleem GangjeeDivision of Medicinal Chemistry, Graduate School of Pharmaceutical Sciences, Duquesne University, 600 Forbes Avenue, Pittsburgh, PA 15282, United States. gangjee@duq.edu
Ying Zhao
Michael A Ihnat
Jessica E Thorpe
Lora C Bailey-Downs
Roy L Kisliuk
University of Oklahoma Health Sciences Center · USDuquesne University · USTufts University · US

Funding

Novel Single, Dual and Multitargeted Inhibitors of RTKsR01CA098850 · NCI · DUQUESNE UNIVERSITY · PI GANGJEE, ALEEM · 2003 to 2007
$1.4M
NCI NIH HHS CA 098850NCI NIH HHS R01 CA098850
6 · The paper itself

Abstract

We designed, synthesized and evaluated 13 novel tricyclic indeno[2,1-d]pyrimidines as RTK inhibitors. These analogues were synthesized via a Dieckmann condensation of 1,2-phenylenediacetonitrile followed by cyclocondensation with guanidine carbonate to afford the 2-amino-3,9-dihydro-indeno[2,1-d]pyrimidin-4-one. Sulfonation of the 4-position followed by displacement with appropriately substituted anilines afforded the target compounds. These compounds were potent inhibitors of platelet-derived growth factor receptor β (PDGFRβ) and inhibited angiogenesis in the chicken embryo chorioallantonic membrane (CAM) assay compared to standards. In addition, compound 7 had a two digit nanomolar GI(50) against nine tumor cell lines, a submicromolar GI(50) against 29 of other tumor cell lines in the preclinical NCI 60 tumor cell line panel. Compound 7 also demonstrated significant in vivo inhibition of tumor growth and angiogenesis in a B16-F10 syngeneic mouse melanoma model.

Indexed as

Angiogenesis InhibitorsAnimalsAntineoplastic AgentsCell Line, TumorCell ProliferationChick EmbryoDrug Screening Assays, AntitumorHumansIndenesMelanoma, ExperimentalMicePyrimidinesReceptor, Platelet-Derived Growth Factor beta(4-chlorophenyl)-9H-indeno(2,1-d)pyrimidine-2,4-diamineAngiogenesis InhibitorsAntineoplastic AgentsIndenesPyrimidinesReceptor, Platelet-Derived Growth Factor beta

Identifiers

PMID22739090
PMCPMC3397428
OpenAlexW2083514272

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.