Evidence map›Paper›PMID 22480849›Full record

ArticleBioorganic & medicinal chemistry2012

Structural modifications modulate stability of glutathione-activated arylated diazeniumdiolate prodrugs.

Rahul S Nandurdikar, Anna E Maciag, Ryan J Holland, Zhao Cao, Paul J Shami, Lucy M Anderson, Larry K Keefer, Joseph E Saavedra

Abstract 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 5 papers.

0numbers the graph read from it
0cells of the map it votes in
5citing 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

5 citing papers in PubMed.

  1. Click chemistry and drug delivery: A bird's-eye view.Acta pharmaceutica Sinica. B · 2023
    Review
  2. Article
  3. Article
  4. Article
  5. 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

8 authors.

Rahul S NandurdikarDrug Design Section, Chemical Biology Laboratory, National Cancer Institute at Frederick, Frederick, MD 21702, USA. nandurdikarr@mail.nih.gov
Anna E Maciag
Ryan J Holland
Zhao Cao
Paul J Shami
Lucy M Anderson
Larry K Keefer
Joseph E Saavedra

Funding

Using Diazeniumdiolate Chemistry to Design Nitric Oxide-Based TherapiesZIABC005673 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI KEEFER, LARRY K · 2009 to 2015
$5.5M
Diazeniumdiolates as Broad-Spectrum Anticancer AgentsZIABC011188 · NCI · DIVISION OF BASIC SCIENCES - NCI · PI KEEFER, LARRY K · 2009 to 2015
$5.2M
CCR NIH HHS HHSN261200800001CIntramural NIH HHS Z99 CA999999NCI NIH HHS HHSN261200800001ENCI NIH HHS Y99 CA999999
6 · The paper itself

Abstract

JS-K, a diazeniumdiolate-based nitric oxide (NO)-releasing prodrug, is currently in late pre-clinical development as an anti-cancer drug candidate. This prodrug was designed to be activated by glutathione (GSH) to release NO. To increase the potency of JS-K, we are investigating the effect of slowing the reaction of the prodrugs with GSH. Herein, we report the effect of replacement of nitro group(s) by other electron-withdrawing group(s) in JS-K and its homo-piperazine analogues on GSH activation and the drugs' biological activity. We show that nitro-to-cyano substitution increases the half-life of the prodrug in the presence of GSH without compromising the compound's in vivo antitumor activity.

Indexed as

AnimalsAntineoplastic AgentsApoptosisAzo CompoundsDrug StabilityGlutathioneHalf-LifeHumansJNK Mitogen-Activated Protein KinasesKineticsMiceNeoplasmsNitric OxideProdrugsSignal TransductionAntineoplastic AgentsAzo CompoundsdiazeniumdiolateGlutathioneJNK Mitogen-Activated Protein KinasesNitric OxideProdrugs

Identifiers

PMID22480849
PMCPMC3590845

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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.