Synthesis and Anticancer Evaluation of PCNA Inhibitor AOH1996 Analogs in Cancer Cell Cultures.

Simona Jonušienė, Agnė Janonienė, Mantas Jonušis, Adas Darinskas, Denis Sokol

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In one paragraph

Article in Molecules (Basel, Switzerland), 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Not yet cited in PubMed.

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1 · What the graph read from it

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2 · The registry

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4 · The record

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5 · Who and what money

Authors and funding

5 authors.

Simona JonušienėFaculty of Chemistry and Geosciences, Institute of Chemistry, Vilnius University, Naugarduko g. 24, LT-03225 Vilnius, Lithuania.ORCID 0009-0004-7074-028X

Agnė JanonienėLife Sciences Center, Institute of Biotechnology, Vilnius University, Saulėtekio g. 7, LT-10257 Vilnius, Lithuania.

Mantas JonušisLife Sciences Center, Institute of Biochemistry, Vilnius University, Mokslininkų g. 12A, LT-08412 Vilnius, Lithuania.ORCID 0000-0003-0045-5542

Adas DarinskasLaboratory of Immunology, National Cancer Institute, P. Baublio g. 3b, LT-08406 Vilnius, Lithuania.

Denis SokolFaculty of Chemistry and Geosciences, Institute of Chemistry, Vilnius University, Naugarduko g. 24, LT-03225 Vilnius, Lithuania.

Funding

No grant is acknowledged in the PubMed record.

6 · The paper itself

Abstract

Proliferating cell nuclear antigen (PCNA) is a critical regulator of DNA replication and repair, and its cancer-associated isoforms represent promising therapeutic targets. The small molecule AOH1996 has been previously reported as a PCNA inhibitor with potent antiproliferative activity. Here, a series of novel AOH1996-based structural analogs were synthesized using structure-activity relationship (SAR) and scaffold-hopping strategies, including 1,2,3-triazole, glycine, and amide derivatives with diverse aromatic and polar substituents. The antiproliferative activity of these compounds was evaluated in MCF-7 (breast cancer) and U87 (glioblastoma) cell lines using the MTT assay. The parent compound AOH1996 exhibited the strongest cytotoxicity, reducing cell viability below 30% at 10 μM. Among the analogs, compounds

Indexed as

Antineoplastic AgentsProliferating Cell Nuclear AntigenCell Line, TumorCell ProliferationCell SurvivalDrug Screening Assays, AntitumorHumansMCF-7 CellsMolecular StructureStructure-Activity RelationshipTriazolesAntineoplastic AgentsPCNA protein, humanProliferating Cell Nuclear AntigenTriazolesADMET predictionanticancer activityAOH1996 analogscytotoxicityMCF-7PCNA inhibitorstructure–activity relationshipU87

Identifiers

PMID41828847

DOI10.3390/molecules31050862

PMCPMC12985466

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