Evidence map›Paper›PMID 36559094›Full record

ArticlePharmaceutics2022

Discovery of 1-Benzhydryl-Piperazine-Based HDAC Inhibitors with Anti-Breast Cancer Activity: Synthesis, Molecular Modeling, In Vitro and In Vivo Biological Evaluation.

Dusan Ruzic, Bernhard Ellinger, Nemanja Djokovic, Juan F Santibanez, Sheraz Gul, Milan Beljkas, Ana Djuric, Arasu Ganesan, Aleksandar Pavic, Tatjana Srdic-Rajic and 2 more

Open access · goldAbstract read
In one paragraph

Article in Pharmaceutics, 2022. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 11 papers.

0numbers the graph read from it
0cells of the map it votes in
11citing papers in PubMed
1.4field-weighted citation impact, top 19% of its field
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

11 citing papers in PubMed, 16 citations in OpenAlex.

  1. Piperazine derivatives as anticancer agents: a medicinal chemistry review of structure, mechanism, and clinical translation.Medicinal chemistry research : an international journal for rapid communications on design and mechanisms of action of biologically active agents · 2026
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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

12 authors at 4 institutions in 4 countries.

Dusan RuzicDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.ORCID 0000-0002-0546-8265
Bernhard EllingerFraunhofer Institute for Translational Medicine and Pharmacology (ITMP), 22525 Hamburg, Germany.
Nemanja DjokovicDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.ORCID 0000-0001-9972-3492
Juan F SantibanezGroup for Molecular Oncology, Institute for Medical Research, University of Belgrade, Dr. Subotića 4, 11129 Belgrade, Serbia.ORCID 0000-0001-9951-8990
Sheraz GulFraunhofer Institute for Translational Medicine and Pharmacology (ITMP), 22525 Hamburg, Germany.ORCID 0000-0003-2543-1643
Milan BeljkasDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Ana DjuricDepartment of Experimental Oncology, Institute for Oncology and Radiology of Serbia, Pasterova 14, 11000 Belgrade, Serbia.ORCID 0000-0002-4440-9890
Arasu GanesanSchool of Pharmacy, University of East Anglia, Norwich Research Park, Norwich NR4 7TJ, UK.ORCID 0000-0003-4862-7999
Aleksandar PavicInstitute of Molecular Genetics and Genetic Engineering, University of Belgrade, Vojvode Stepe 444a, 11000 Belgrade, Serbia.ORCID 0000-0003-3233-1341
Tatjana Srdic-RajicDepartment of Experimental Oncology, Institute for Oncology and Radiology of Serbia, Pasterova 14, 11000 Belgrade, Serbia.
Milos PetkovicDepartment of Organic Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
Katarina NikolicDepartment of Pharmaceutical Chemistry, Faculty of Pharmacy, University of Belgrade, Vojvode Stepe 450, 11221 Belgrade, Serbia.
University of Belgrade · RSFraunhofer Institute for Translational Medicine and Pharmacology · DEOncology Institute of Vojvodina · RSUniversity of East Anglia · GB

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Isoform-selective histone deacetylase (HDAC) inhibition is promoted as a rational strategy to develop safer anti-cancer drugs compared to non-selective HDAC inhibitors. Despite this presumed benefit, considerably more non-selective HDAC inhibitors have undergone clinical trials. In this report, we detail the design and discovery of potent HDAC inhibitors, with 1-benzhydryl piperazine as a surface recognition group, that differ in hydrocarbon linker. In vitro HDAC screening identified two selective HDAC6 inhibitors with nanomolar IC

Indexed as

1-benzhydryl piperazineanti-metastatic effectbreast cancerdrug discoveryhistone deacetylaseshydroxamic acidzebrafish xenograft model

Identifiers

PMID36559094
PMCPMC9785542
OpenAlexW4310223453

What OpenQuestion holds

Textmetadata
LicenceCC BY
Read underepoch 390

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.