Evidence map›Paper›PMID 39885716›Full record

ArticleFuture medicinal chemistry2025

Pioneering first-in-class HDAC-ROCK inhibitors as potential multitarget anticancer agents.

Milan Beljkas, Dusan Ruzic, Ana Djuric, Ana Vuletic, Guilaine Nchugoua Tchiehe, Corinne Jallet, Véronique Cadet-Daniel, Paola B Arimondo, Juan F Santibanez, Tatjana Srdic-Rajic and 3 more

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Article in Future medicinal chemistry, 2025. 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

13 authors.

Milan BeljkasDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
Dusan RuzicDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.
Ana DjuricDepartment of Experimental Oncology, Institute for Oncology and Radiology of Serbia, Belgrade, Serbia.ORCID 0000-0002-4440-9890
Ana VuleticDepartment of Experimental Oncology, Institute for Oncology and Radiology of Serbia, Belgrade, Serbia.
Guilaine Nchugoua TchieheDepartment of Structural Biology and Chemistry, Epigenetic Chemical Biology, Institut Pasteur, Université Paris Cité, CNRS UMR3523 Chem4Life, Department of Structural Biology and Chemistry, Paris, France.
Corinne JalletDepartment of Structural Biology and Chemistry, Epigenetic Chemical Biology, Institut Pasteur, Université Paris Cité, CNRS UMR3523 Chem4Life, Department of Structural Biology and Chemistry, Paris, France.
Véronique Cadet-DanielDepartment of Structural Biology and Chemistry, Epigenetic Chemical Biology, Institut Pasteur, Université Paris Cité, CNRS UMR3523 Chem4Life, Department of Structural Biology and Chemistry, Paris, France.
Paola B ArimondoDepartment of Structural Biology and Chemistry, Epigenetic Chemical Biology, Institut Pasteur, Université Paris Cité, CNRS UMR3523 Chem4Life, Department of Structural Biology and Chemistry, Paris, France.
Juan F SantibanezGroup for Molecular Oncology, Institute for Medical Research, National Institute of the Republic of Serbia, University of Belgrade, Belgrade, Serbia.ORCID 0000-0001-9951-8990
Tatjana Srdic-RajicDepartment of Experimental Oncology, Institute for Oncology and Radiology of Serbia, Belgrade, Serbia.
Katarina NikolicDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.ORCID 0000-0002-3656-9245
Slavica OljacicDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.ORCID 0000-0001-9128-6072
Milos PetkovicDepartment of Organic Chemistry, Faculty of Pharmacy, University of Belgrade, Belgrade, Serbia.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

aimWith the aim of simultaneously modulating the epigenetic system and the protein kinase pathway, we selected the enzyme histone deacetylase (HDAC) and the Rho-associated protein kinases (ROCK) as desired targets to develop potential multitarget anticancer agents with additional antimetastatic properties. We report here the rational design, synthesis, and biological evaluation of the MATERIALS AND

methodsA molecular docking study performed with the Gold software was used to develop HDAC/ROCK multitarget inhibitors. IC

results

conclusionThe findings of this study strongly suggest that the simultaneous inhibition of ROCK and HDACs holds significant potential as a promising therapeutic strategy in the advancement of cancer treatment.

Indexed as

Antineoplastic AgentsHistone Deacetylase InhibitorsHistone DeacetylasesProtein Kinase Inhibitorsrho-Associated KinasesCell Line, TumorCell MovementCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMolecular Docking SimulationMolecular StructurePancreatic NeoplasmsStructure-Activity RelationshipAntineoplastic AgentsHistone Deacetylase InhibitorsHistone DeacetylasesProtein Kinase Inhibitorsrho-Associated KinasesROCK1 protein, humanbreast cancerHistone deacetylasemultitarget‐directed ligandspancreatic ductal adenocarcinomaRho-associated protein kinases

Identifiers

PMID39885716
PMCPMC11834526

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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.