Evidence map›Paper›PMID 21493066›Full record

ArticleBioorganic & medicinal chemistry letters2011

Development of tricyclic hydroxy-1H-pyrrolopyridine-trione containing HIV-1 integrase inhibitors.

Xue Zhi Zhao, Kasthuraiah Maddali, Mathieu Metifiot, Steven J Smith, B Christie Vu, Christophe Marchand, Stephen H Hughes, Yves Pommier, Terrence R Burke

Abstract read
In one paragraph

Article in Bioorganic & medicinal chemistry letters, 2011. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 7 papers.

0numbers the graph read from it
0cells of the map it votes in
7citing 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

7 citing papers in PubMed.

  1. Article
  2. Article
  3. An Overview of the Biological Activity of Pyrrolo[3,4-Pharmaceuticals (Basel, Switzerland) · 2021
    Review
  4. Review
  5. Article
  6. Article
  7. Review
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.

Xue Zhi ZhaoChemical Biology Laboratory, Molecular Discovery Program, Center for Cancer Research, National Cancer Institute-Frederick, National Institutes of Health, Frederick, MD 21702, USA. xuezhi.zhao@nih.gov
Kasthuraiah Maddali
Mathieu Metifiot
Steven J Smith
B Christie Vu
Christophe Marchand
Stephen H Hughes
Yves Pommier
Terrence R Burke

Funding

IntegraseZIABC011426 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI HUGHES, STEPHEN H · 2012 to 2022
$14.0M
Design and Synthesis of HIV Integrase as Potential Anti-AIDS DrugsZIABC007363 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI BURKE, TERRENCE · 2009 to 2025
$11.7M
Pharmacology of HIV Viral DNA & Retroviral IntegrasesZIABC007333 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI POMMIER, YVES · 2009 to 2019
$5.2M
Retroviral Replication and Vector DesignZIABC010482 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI HUGHES, STEPHEN H · 2009 to 2011
$3.7M
Intramural NIH HHS Z99 CA999999Intramural NIH HHS ZIA BC007363
6 · The paper itself

Abstract

New tricyclic HIV-1 integrase (IN) inhibitors were prepared that combined structural features of bicyclic pyrimidinones with recently disclosed 4,5-dihydroxy-1H-isoindole-1,3(2H)-diones. This combination resulted in the introduction of a nitrogen into the aryl ring and the addition of a fused third ring to our previously described inhibitors. The resulting analogues showed low micromolar inhibitory potency in in vitro HIV-1 integrase assays, with good selectivity for strand transfer relative to 3'-processing.

Indexed as

Biological AssayCells, CulturedCyclizationHIV-1HIV IntegraseHIV Integrase InhibitorsHumansHydroxylationInhibitory Concentration 50Molecular StructurePyrimidinonesStructure-Activity RelationshipHIV IntegraseHIV Integrase Inhibitorsp31 integrase protein, Human immunodeficiency virus 1Pyrimidinones

Identifiers

PMID21493066
PMCPMC3085635

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.