Evidence map›Paper›PMID 23237838›Full record

ArticleBioorganic & medicinal chemistry letters2013

Synthesis and biological activity of aminophthalazines and aminopyridazines as novel inhibitors of PGE2 production in cells.

Federico Medda, Earlphia Sells, Hui-Hua Chang, Justin Dietrich, Shashi Chappeta, Breland Smith, Vijay Gokhale, Emmanuelle J Meuillet, Christopher Hulme

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 2 papers.

0numbers the graph read from it
0cells of the map it votes in
2citing 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

2 citing papers in PubMed.

  1. Review
  2. Amino- and polyaminophthalazin-1(2Beilstein journal of organic chemistry · 2021
    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

9 authors.

Federico MeddaBIO5 Oro Valley, The University of Arizona, 1580 E. Hanley Blvd., Oro Valley, AZ 85737, USA.
Earlphia Sells
Hui-Hua Chang
Justin Dietrich
Shashi Chappeta
Breland Smith
Vijay Gokhale
Emmanuelle J Meuillet
Christopher Hulme

Funding

VITAMIN AP30CA023074 · NCI · UNIVERSITY OF ARIZONA · PI Dan Theodorescu · 1985 to 2026
$110.2M
GRADUATE TRAINING IN BIOCHEMISTRY AND MOLECULAR BIOLOGYT32GM008659 · NIGMS · UNIVERSITY OF ARIZONA · PI CAPALDI, ANDREW PAUL, WEINERT, TED A. · 1997 to 2019
$5.3M
CHEMISTRY-BIOLOGY INTERFACE TRAINING PROGRAMT32GM008804 · NIGMS · UNIVERSITY OF ARIZONA · PI MONTFORT, WILLIAM R. · 2003 to 2023
$3.9M
Inhibition of novel molecular targets of prostaglandin formation for antitumor acR01CA138702 · NCI · UNIVERSITY OF ARIZONA · PI MEUILLET, EMMANUELLE JOELLE · 2010 to 2014
$1.6M
NCI NIH HHS CA138702NCI NIH HHS R01 CA138702NIGMS NIH HHS 5T32GM008804-09NIGMS NIH HHS T32 GM008659NIGMS NIH HHS T32 GM008804NIGMS NIH HHS T32GM08659
6 · The paper itself

Abstract

This Letter reports the synthesis and biological evaluation of a collection of aminophthalazines as a novel class of compounds capable of reducing production of PGE(2) in HCA-7 human adenocarcinoma cells. A total of 28 analogs were synthesized, assayed for PGE(2) reduction, and selected active compounds were evaluated for inhibitory activity against COX-2 in a cell free assay. Compound 2xxiv (R(1)=H, R(2)=p-CH(3)O) exhibited the most potent activity in cells (EC(50)=0.02 μM) and minimal inhibition of COX-2 activity (3% at 5 μM). Furthermore, the anti-tumor activity of analog 2vii was analyzed in xenograft mouse models exhibiting good anti-cancer activity.

Indexed as

AminopyridinesAnimalsAntineoplastic AgentsCell Line, TumorDinoprostoneDisease Models, AnimalEnzyme ActivationGene Expression RegulationHumansMiceMolecular StructurePhthalazinesTransplantation, Heterologous5-aminophthalazineAminopyridinesAntineoplastic AgentsDinoprostonePhthalazines

Identifiers

PMID23237838
PMCPMC3534862

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.