Identification of New Mono/Dihydroxynaphthoquinone as Lead Agents That Inhibit the Growth of Refractive and Triple-Negative Breast Cancer Cell Lines.
Journal
ACS omega
ISSN: 2470-1343
Titre abrégé: ACS Omega
Pays: United States
ID NLM: 101691658
Informations de publication
Date de publication:
30 Jun 2019
30 Jun 2019
Historique:
received:
02
04
2019
accepted:
15
05
2019
entrez:
29
8
2019
pubmed:
29
8
2019
medline:
29
8
2019
Statut:
epublish
Résumé
Human epidermal growth factor receptor 2 (HER2) is overexpressed in nearly 20-30% of breast cancers and is associated with metastasis resulting in poor patient survival and high recurrence. The dual EGFR/HER2 kinase inhibitor lapatinib has shown promising clinical results, but its limitations have also led to the resistance and activation of tumor survival pathways. Following our previous investigation of quinones as HER2 kinase inhibitors, we synthesized several naphthoquinone derivatives that significantly inhibited breast tumor cells expressing HER2 and trastuzumab-resistant HER2 oncogenic isoform, HER2Δ16. Two of these compounds were shown to be more effective than lapatinib at the inhibition of HER2 autophosphorylation of Y1248. Compounds
Identifiants
pubmed: 31460159
doi: 10.1021/acsomega.9b00929
pmc: PMC6648266
doi:
Types de publication
Journal Article
Langues
eng
Pagination
10610-10619Subventions
Organisme : NIMHD NIH HHS
ID : G12 MD007595
Pays : United States
Organisme : NIGMS NIH HHS
ID : P20 GM103424
Pays : United States
Organisme : NIMHD NIH HHS
ID : U54 MD007595
Pays : United States
Déclaration de conflit d'intérêts
The authors declare no competing financial interest.
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