ArticleMolecular diversity2026
Discovery of novel quinazoline derivatives containing trifluoromethyl against cell proliferation by targeting werner helicase.
Article in Molecular diversity, 2026. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 4 papers.
What it found
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Who cites it
4 citing papers in PubMed.
- A trifluoromethyl quinazoline inhibits hepatocellular carcinoma proliferation through HDAC1 binding and multi-target mechanisms.iScience · 2026Article
- NAT10 and ac4C modification in cancer immunity and metabolism: emerging mechanisms and therapeutic potential.Journal of translational medicine · 2026Review
- A Trifluoromethyl Quinazoline Compound Regulates the Epithelial-Mesenchymal Transition of Prostatic Hyperplasia Cells by Inhibiting the Secretion of TGF-β1 in Stromal Cells.Current issues in molecular biology · 2025Article
- Quinazoline Derivative kzl052 Suppresses Prostate Cancer by Targeting WRN Helicase to Stabilize DNA Replication Forks.International journal of molecular sciences · 2025Article
Corrections and comments
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Authors and funding
13 authors.
Funding
No grant is acknowledged in the PubMed record.
Abstract
A series of novel 2-trifluoromethyl-4-aminoquinazoline derivatives were designed and synthesized, and their antitumor activities were evaluated. Among them, several target compounds exhibited nanomolar inhibitory activities against K562 and LNCaP. Meanwhile, the results of in vitro and in vivo activity evaluation showed that compound 9 had the significant selective anticancer activity and the lower toxicity. The target prediction and pathway analysis showed that the mechanism of compound 9 on the proliferation inhibitory activity of K562 and PC3 cells may be via inhibiting werner helicase (WRN) activity and affecting DNA damage repair. As expected, biological evaluation showed that compound 9 bind to WRN, significantly downregulated the expression of WRN, inhibited the MDM2/p53 pathway, to render the damaged DNA unrepaired, eventually causing mitotic arrest and cell death. Our findings provide a foundation for further research of trifluoromethyl-quinazoline-4-amines as WRN-dependent anticancer agents that targeting DNA damage repair pathway.
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Registered trials
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