Evidence map›Paper›PMID 41518355›Full record

ArticleArchiv der Pharmazie2026

New Quinoline Kinase Inhibitors With Good Selectivity for NAK Kinases and Anti-Tumor Activity Against Ewing Sarcoma.

Caroline de Bem Gentz, Thais Helena Maciel Fernandes, Marcela Silva Lopes, Lewis Elson, Andreas Krämer, Lucas Rodrigo de Souza, Isadora Serraglio Fortes, Geórgia Silva Pinto, Martha Cestari Silva Martins, Henrique Barros de Lima and 8 more

Abstract read
PubMed Full text at PMC Publisher
In one paragraph

Article in Archiv der Pharmazie, 2026. 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. 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

18 authors.

Caroline de Bem GentzPharmaceutical Sciences Graduate Program, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
Thais Helena Maciel FernandesPharmaceutical Sciences Graduate Program, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
Marcela Silva LopesDepartment of Pharmacology, Institute of Basic Health Sciences, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
Lewis ElsonInstitute of Pharmaceutical Chemistry, Goethe University, Frankfurt, am Main, Germany.
Andreas KrämerInstitute of Pharmaceutical Chemistry, Goethe University, Frankfurt, am Main, Germany.
Lucas Rodrigo de SouzaCenter for Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas (UNICAMP), Campinas, São Paulo, Brazil.
Isadora Serraglio FortesPharmaceutical Sciences Graduate Program, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
Geórgia Silva PintoPharmaceutical Synthesis Group (PHARSG), School of Pharmacy, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
Martha Cestari Silva MartinsPharmaceutical Sciences Graduate Program, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
Henrique Barros de LimaPharmaceutical Sciences Graduate Program, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
André da Silva SantiagoCenter for Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas (UNICAMP), Campinas, São Paulo, Brazil.
Lauro José GregianinNational Science and Technology Institute for Children's Cancer Biology and Pediatric Oncology - INCT BioOncoPed, Porto Alegre, Brazil.
Katlin Brauer MassirerCenter for Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas (UNICAMP), Campinas, São Paulo, Brazil.
Mário Henrique BengtsonCenter for Medicinal Chemistry (CQMED), Center for Molecular Biology and Genetic Engineering (CBMEG), University of Campinas (UNICAMP), Campinas, São Paulo, Brazil.
Rafael RoeslerDepartment of Pharmacology, Institute of Basic Health Sciences, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.
Stefan KnappInstitute of Pharmaceutical Chemistry, Goethe University, Frankfurt, am Main, Germany.
Stefan A LauferDepartment of Pharmaceutical and Medicinal Chemistry, Institute of Pharmaceutical Sciences, University of Tübingen, Tübingen, Germany.
Saulo Fernandes de AndradePharmaceutical Sciences Graduate Program, Universidade Federal do Rio Grande do Sul (UFRGS), Porto Alegre, Rio Grande do Sul, Brazil.ORCID https://orcid.org/0000-0003-2873-7939

Funding

Conselho Nacional de Desenvolvimento Científico e Tecnológico 307104/2025-7Conselho Nacional de Desenvolvimento Científico e Tecnológico 406484/2022-8Conselho Nacional de Desenvolvimento Científico e Tecnológico 446573/2025-6Coordenação de Aperfeiçoamento de Pessoal de Nível Superior Finance Code 001EUbOPEN 875510Frankfurt Cancer InstituteFundação de Amparo à Pesquisa do Estado de São Paulo 2013/50724-5Fundação de Amparo à Pesquisa do Estado de São Paulo 2014/50897-0Fundação de Amparo à Pesquisa do Estado de São Paulo 2020/16094-8Fundação de Amparo à Pesquisa do Estado de São Paulo 2024/09297-0Fundação de Amparo à Pesquisa do Estado do R.S. 24/2551-0001376-8Structural Genomics Consortium 1097737
6 · The paper itself

Abstract

In the past few years, several novel anticancer agents targeting protein kinases have been discovered expanding the available therapeutic arsenal. However, few new therapeutic approaches have been developed for the treatment of childhood cancer. To this end, we have been making efforts to contribute to this important field. Herein, we identified a series of new 4,6-disubstituted quinoline derivatives from our in-house quinoline chemical library that showed promising anti-proliferative activity against Ewing Sarcoma (ES). This interesting observation engaged us to further investigate these derivatives since this type of cancer is among the most common bone cancers in children. Evaluation of the quinoline derivatives against a panel of kinases demonstrated generally narrow selectivity profiles of this compound class. Interestingly, the main kinases that were inhibited belonged to the NAK family of kinases, in particular, the family member cyclin G-associated kinase (GAK) which was inhibited at nanomolar range in enzyme kinetic assays.

Indexed as

Antineoplastic AgentsBone NeoplasmsProtein Kinase InhibitorsQuinolinesSarcoma, EwingCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMolecular StructureStructure-Activity RelationshipAntineoplastic AgentsProtein Kinase InhibitorsQuinolinesEwing SarcomaGAKinhibitorpanel of kinasesquinoline

Identifiers

PMID41518355
PMCPMC12790329

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Registered trials

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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.