Evidence map›Paper›PMID 39361055›Full record

ReviewJournal of medicinal chemistry2024

Geldanamycin, a Naturally Occurring Inhibitor of Hsp90 and a Lead Compound for Medicinal Chemistry.

Russell R A Kitson, Dominika Kitsonová, David Siegel, David Ross, Christopher J Moody

Abstract readReview
In one paragraph

Review in Journal of medicinal chemistry, 2024. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 10 papers.

0numbers the graph read from it
0cells of the map it votes in
10citing 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

10 citing papers in PubMed.

  1. Article
  2. Review
  3. International journal of molecular sciences · 2025
    Article
  4. Article
  5. Phytochemicals fromMicroorganisms · 2025
    Article
  6. Review
  7. Review
  8. Article
  9. Review
  10. 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

5 authors.

Russell R A KitsonDepartment of Organic and Bioorganic Chemistry, Charles University, Faculty of Pharmacy in Hradec Králové, Akademika Heyrovského 1203, 50005 Hradec Králové, Czech Republic.
Dominika KitsonováDatwyler Sealing Technologies CZ Ltd., Polní 224, 50401 Nový Bydžov, Czech Republic.
David SiegelDepartment of Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus, 12850 East Montview Boulevard, Aurora, Colorado 80045, United States.
David RossDepartment of Pharmaceutical Sciences, University of Colorado Anschutz Medical Campus, 12850 East Montview Boulevard, Aurora, Colorado 80045, United States.
Christopher J MoodySchool of Chemistry, University of Nottingham, University Park, Nottingham NG7 2RD, U.K.ORCID 0000-0003-0487-041X

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Geldanamycin remains a driver in the medicinal chemistry of heat shock protein 90 (Hsp90) inhibition, even half a century after its original isolation from nature. This Perspective focuses on the properties of the benzoquinone ring of the natural product that enable a range of functionalization reactions to take place. Therefore, inherent reactivity at C-17, where the methoxy group serves as a vinylogous ester, and at C-19 that demonstrates nucleophilic, enamide-type character toward electrophiles, and also as a conjugate acceptor to react with nucleophiles, has facilitated the synthesis of semisynthetic derivatives. Thus, a range of C-17-substituted amine derivatives has been investigated in oncology applications, with a number of compounds in this series reaching clinical trials. In contrast, the 19-position of geldanamycin has received less attention, although 19-substituted derivatives offer promise with markedly reduced toxicity compared to geldanamycin itself, while retaining Hsp90 inhibitory activity albeit with diminished potency in cellular studies.

Indexed as

BenzoquinonesHSP90 Heat-Shock ProteinsLactams, MacrocyclicAnimalsAntineoplastic AgentsChemistry, PharmaceuticalHumansStructure-Activity RelationshipAntineoplastic AgentsBenzoquinonesgeldanamycinHSP90 Heat-Shock ProteinsLactams, Macrocyclic

Identifiers

PMID39361055
PMCPMC11513894

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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.