Evidence map›Paper›PMID 41334934›Full record

ArticleArchiv der Pharmazie2025

Design, Synthesis, and Selective Antiproliferative Activity of Indolizine Derivatives as Microtubule Destabilizers.

Victor Hugo Catricala Fernandes, Maitê Bueno Giometti, Franco Jazon Caires, Gabriel de Paula Bueno, Gabriel da Silva, Andréia Machado Leopoldino, Anna Junker, Giuliano Cesar Clososki

Abstract read
In one paragraph

Article in Archiv der Pharmazie, 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. 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.

Victor Hugo Catricala FernandesDepartment of Biomolecular Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of Sao Paulo, Ribeirão Preto, Brazil.ORCID https://orcid.org/0000-0001-8423-9454
Maitê Bueno GiomettiDepartment of Biomolecular Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of Sao Paulo, Ribeirão Preto, Brazil.
Franco Jazon CairesDepartment of Biomolecular Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of Sao Paulo, Ribeirão Preto, Brazil.ORCID https://orcid.org/0000-0002-4579-6837
Gabriel de Paula BuenoDepartment of Biomolecular Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of Sao Paulo, Ribeirão Preto, Brazil.
Gabriel da SilvaDepartment of Clinical Analyses, Toxicological and Food Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of Sao Paulo, Ribeirão Preto, Brazil.
Andréia Machado LeopoldinoDepartment of Clinical Analyses, Toxicological and Food Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of Sao Paulo, Ribeirão Preto, Brazil.
Anna JunkerWerner Siemens Imaging Center, Department of Preclinical Imaging and Radiopharmacy, Cluster of Excellence iFIT (EXC 2180) "Image-guided and Functionally Instructed Tumor Therapies", University of Tuebingen, Tuebingen, Germany.
Giuliano Cesar ClososkiDepartment of Biomolecular Sciences, Faculty of Pharmaceutical Sciences of Ribeirão Preto, University of Sao Paulo, Ribeirão Preto, Brazil.

Funding

The authors gratefully acknowledge financial support for this study by the Brazilian foundations Fundação de Amparo à Pesquisa do Estado de São Paulo (FAPESP, Grants 2022/06051-5, 2023/09624-9, 2022/14888-2, and 2022/05327-7), Conselho Nacional de Desenvolvimento Científico e Tecnológico (CNPq), Coordenação de Aperfeiçoamento de Pessoal de Nível Superior (CAPES, Finance Code 001), and Universidade de São Paulo (USP). A.J. thanks the German Research Foundation (DFG) for the financial support (EXC 2180-390900677).
6 · The paper itself

Abstract

The development of selective anticancer agents with minimal off-target toxicity remains a major therapeutic goal. In this study, we synthesized and evaluated a series of 32 indolizine derivatives for antiproliferative activity against oral (CAL-27), breast (BT-20), and gastric (HGC-27) cancer cell lines, as well as non-tumoral fibroblasts (OHMF). Compounds 8e and 8h emerged as potent and selective candidates, exhibiting nanomolar IC₅₀ values (47-117 nM) and negligible cytotoxicity toward healthy cells. These compounds induced G2/M cell-cycle arrest, inhibited tubulin polymerization, and modulated proteins related to apoptosis and proliferation, including p-AKT, cyclin D1, Bcl-2, and p21. Docking studies confirmed their interaction with the colchicine-binding site of tubulin. Together, the results support further investigation of these compounds as microtubule-interacting agents with selective antiproliferative activity.

Indexed as

Antineoplastic AgentsDrug DesignIndolizinesMicrotubulesTubulin ModulatorsApoptosisCell Line, TumorCell ProliferationDose-Response Relationship, DrugDrug Screening Assays, AntitumorHumansMolecular Docking SimulationMolecular StructureStructure-Activity RelationshipTubulinAntineoplastic AgentsindolizineIndolizinesTubulinTubulin Modulatorsantiproliferativebioisosteric exchangeindolizinemolecular dockingtubulin inhibitor

Identifiers

PMID41334934
PMCPMC12673918

What OpenQuestion holds

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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.