Evidence map›Paper›PMID 21641218›Full record

ArticleBioorganic & medicinal chemistry letters2011

Synthesis, transport and antiviral activity of Ala-Ser and Val-Ser prodrugs of cidofovir.

Larryn W Peterson, Jae-Seung Kim, Paul Kijek, Stefanie Mitchell, John Hilfinger, Julie Breitenbach, Kathy Borysko, John C Drach, Boris A Kashemirov, Charles E McKenna

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. Mpox (formerly monkeypox): pathogenesis, prevention, and treatment.Signal transduction and targeted therapy · 2023
    Review
  2. Review
  3. Review
  4. Article
  5. Article
  6. Article
  7. Cytomegalovirus antivirals and development of improved animal models.Expert opinion on drug metabolism & toxicology · 2011
    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

10 authors.

Larryn W PetersonDepartment of Chemistry, University of Southern California, Los Angeles, CA 90089-0744, USA.
Jae-Seung Kim
Paul Kijek
Stefanie Mitchell
John Hilfinger
Julie Breitenbach
Kathy Borysko
John C Drach
Boris A Kashemirov
Charles E McKenna

Funding

Oral Antiviral Prodrugs for Biodefense InitiativeU01AI061457 · NIAID · TSRL, INC. · PI HILFINGER, JOHN M · 2005 to 2009
$5.3M
Novel prodrugs for treatment of human CMV infectionR43AI091216 · NIAID · TSRL, INC. · PI HILFINGER, JOHN M · 2010 to 2011
$591k
NIAID NIH HHS AI061457NIAID NIH HHS AI091216NIAID NIH HHS R43 AI091216NIAID NIH HHS U01 AI061457
6 · The paper itself

Abstract

We report the synthesis and biological evaluation of Ala-(Val-)l-Ser-CO(2)R prodrugs of 1, where a dipeptide promoiety is conjugated to the P(OH)(2) group of cidofovir (1) via esterification by the Ser side chain hydroxyl group and an ethyl group (4 and 5) or alone (6 and 7). In a murine model, oral administration of 4 or 5 did not significantly increase total cidofovir species in the plasma compared to 1 or 2, but 7 resulted in a 15-fold increase in a rat model and had an in vitro EC(50) value against human cytomegalovirus comparable to 1. Neither 6 nor 7 exhibited toxicity up to 100 μM in KB or HFF cells.

Indexed as

Administration, OralAlanineAnimalsAntiviral AgentsCells, CulturedCidofovirCytomegalovirusCytosineDisease Models, AnimalDose-Response Relationship, DrugHumansInhibitory Concentration 50Molecular StructureOrganophosphonatesPeptidesProdrugsAlanineAntiviral AgentsCidofovirCytosineOrganophosphonatesPeptidesProdrugsSerineValine

Identifiers

PMID21641218
PMCPMC3115518

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.