ArticleACS medicinal chemistry letters2013
Synthesis and Evaluation of Quinazolone Derivatives as a New Class of c-KIT G-Quadruplex Binding Ligands.
Article in ACS medicinal chemistry letters, 2013. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 15 papers.
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Who cites it
15 citing papers in PubMed, 49 citations in OpenAlex.
- Selective Delivery of Anticancer Natural G-Quadruplex Ligands by the AT11 Aptamer for Gastric Cancer Treatment.Journal of medicinal chemistry · 2026Article
- G-Quadruplexes in Tumor Immune Regulation: Molecular Mechanisms and Therapeutic Prospects in Gastrointestinal Cancers.Biomedicines · 2025Review
- Two rhenium compounds with benzimidazole ligands: synthesis and DNA interactions.RSC advances · 2024Article
- Asymmetric triplex metallohelices stabilise DNA G-quadruplexes in promoter oncogene sequences and efficiently reduce their expression in cancer cells.Journal of enzyme inhibition and medicinal chemistry · 2023Article
- Application of G-quadruplex targets in gastrointestinal cancers: Advancements, challenges and prospects.World journal of gastrointestinal oncology · 2023Review
- Quadruplex Ligands in Cancer Therapy.Cancers · 2021Review
- Recent Developments in Small-Molecule Ligands of Medicinal Relevance for Harnessing the Anticancer Potential of G-Quadruplexes.Molecules (Basel, Switzerland) · 2021Review
- Stabilization of c-KIT G-Quadruplex DNA Structures by the RNA Polymerase I Inhibitors BMH-21 and BA-41.International journal of molecular sciences · 2019Article
- Recent Progress of Targeted G-Quadruplex-Preferred Ligands Toward Cancer Therapy.Molecules (Basel, Switzerland) · 2019Review
- Article
- Carbazole Derivatives' Binding to c-KIT G-Quadruplex DNA.Molecules (Basel, Switzerland) · 2018Article
- Natural Alkaloids and Heterocycles as G-Quadruplex Ligands and Potential Anticancer Agents.Molecules (Basel, Switzerland) · 2018Review
- Crystal structure of 3-(4-hy-droxy-phen-yl)-2-[(E)-2-phenyl-ethen-yl]quinazolin-4(3H)-one.Acta crystallographica. Section E, Crystallographic communications · 2016Article
- Extended molecular dynamics of a c-kit promoter quadruplex.Nucleic acids research · 2015Article
- Flexibility and structural conservation in a c-KIT G-quadruplex.Nucleic acids research · 2015Article
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Authors and funding
9 authors at 1 institution in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
The c-KIT G-quadruplex structures are a novel class of attractive targets for the treatment of gastrointestinal stromal tumor (GIST). Herein, a series of new quinazolone derivatives with the expansion of unfused aromatic ring system were designed and synthesized. Subsequent biophysical studies demonstrated that the derivatives with adaptive scaffold could effectively bind to and stabilize c-KIT G-quadruplexes with good selectivity against duplex DNA. More importantly, these ligands further inhibited the transcription and expression of c-KIT gene and exhibited significant cytotoxicity on the GIST cell line HGC-27. Overall, these quinazolone derivatives represent a new class of promising c-KIT G-quadruplex ligands. The experimental results have also reinforced the idea of inhibition of c-KIT expression through targeting c-KIT G-quadruplex DNA.
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