Evidence map›Paper›PMID 24900627›Full record

ArticleACS medicinal chemistry letters2013

Design, Synthesis, and Antiviral Evaluation of Chimeric Inhibitors of HIV Reverse Transcriptase.

Pinar Iyidogan, Todd J Sullivan, Mahendra D Chordia, Kathleen M Frey, Karen S Anderson

Abstract read
In one paragraph

Article in ACS medicinal chemistry letters, 2013. 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
–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

1 citing paper in PubMed.

  1. 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

5 authors.

Pinar IyidoganDepartment of Pharmacology, School of Medicine, Yale University , New Haven, Connecticut 06520, United States.
Todd J SullivanDepartment of Pharmacology, School of Medicine, Yale University , New Haven, Connecticut 06520, United States.
Mahendra D ChordiaChemin Pharma , New Haven, Connecticut 06511, United States.
Kathleen M FreyDepartment of Pharmacology, School of Medicine, Yale University , New Haven, Connecticut 06520, United States.
Karen S AndersonDepartment of Pharmacology, School of Medicine, Yale University , New Haven, Connecticut 06520, United States.

Funding

MECHANISM AND INHIBITION OF HIV REVERSE TRANSCRIPTASER01GM049551 · NIGMS · YALE UNIVERSITY · PI ANDERSON, KAREN S. · 1993 to 2019
$9.0M
Structure activity and structure property relationships for novel anti-HIV agentsF32AI104334 · NIAID · YALE UNIVERSITY · PI FREY, KATHLEEN MARY · 2013 to 2015
$140k
NIAID NIH HHS F32 AI104334NIGMS NIH HHS R01 GM049551
6 · The paper itself

Abstract

In a continuing study of potent bifunctional anti-HIV agents, we rationally designed a novel chimeric inhibitor utilizing thymidine (THY) and a TMC derivative (a diarylpyrimidine NNRTI) linked via a polymethylene linker (ALK). The nucleoside, 5'-hydrogen-phosphonate (H-phosphonate), and 5'-triphosphate forms of this chimeric inhibitor (THY-ALK-TMC) were synthesized and the antiviral activity profiles were evaluated at the enzyme and cellular level. The nucleoside triphosphate (11) and the H-phosphonate (10) derivatives inhibited RT polymerization with an IC50 value of 6.0 and 4.3 nM, respectively. Additionally, chimeric nucleoside (9) and H-phosphonate (10) derivatives reduced HIV replication in a cell-based assay with low nanomolar antiviral potencies.

Indexed as

HIVNNRTInucleoside H-phosphonatereverse transcriptasesynthesis

Identifiers

PMID24900627
PMCPMC4027223

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.