ArticleJournal of advanced research2025
Hybridization-based discovery of novel quinazoline-2-indolinone derivatives as potent and selective PI3Kα inhibitors.
Article in Journal of advanced research, 2025. The graph could read no effect estimate from its abstract, so it casts no vote on the map. Cited by 14 papers.
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Who cites it
14 citing papers in PubMed, 54 citations in OpenAlex.
- Identification of novel PI3Kα inhibitors for colon cancer treatment via virtual screening, molecular dynamics simulation, and in vitro activity validation.Molecular diversity · 2026Article
- Engineering selective PI3KActa pharmaceutica Sinica. B · 2026Article
- Mitochondrial metabolism and cancer therapeutic innovation.Signal transduction and targeted therapy · 2025Review
- Responsive ROS-Augmented Prodrug Hybridization Nanoassemblies for Multidimensionally Synergitic Treatment of Hepatocellular Carcinoma in Cascade Assaults.Advanced science (Weinheim, Baden-Wurttemberg, Germany) · 2025Article
- Activity-based protein profiling guided new target identification of quinazoline derivatives for expediting bactericide discovery: Activity-based protein profiling derived new target discovery of antibacterial quinazolines.Journal of advanced research · 2025Article
- An insight into theFuture medicinal chemistry · 2025Review
- Recent advances in the investigation of the quinazoline nucleus and derivatives with potential anticancer activities.Future medicinal chemistry · 2025Review
- The antibreast cancer therapeutic potential of quinazoline hybrids-Part I.Future medicinal chemistry · 2025Review
- 5-Methylcytosine RNA modification and its roles in cancer and cancer chemotherapy resistance.Journal of translational medicine · 2025Review
- Development of indole hybrids for potential lung cancer treatment-part I: nitrogen-containing six-membered aromatic heterocycles.Future medicinal chemistry · 2025Review
- In Vitro Enzymatic and Computational Assessments of Pyrazole-Isatin and Pyrazole-Indole Conjugates as Anti-Diabetic, Anti-Arthritic, and Anti-Inflammatory Agents.Pharmaceutics · 2025Article
- Aptamer-functionalized triptolide with release controllability as a promising targeted therapy against triple-negative breast cancer.Journal of experimental & clinical cancer research : CR · 2024Article
- N-heterocyclic carbene catalyzed [2 + 3] annulation reaction for the synthesis of trifluoroethyl 3,2'-spirooxindole γ-lactam.RSC advances · 2024Article
- Therapeutic potential of flavonoids from traditional Chinese medicine in pancreatic cancer treatment.Frontiers in nutrition · 2024Review
Corrections and comments
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Authors and funding
15 authors at 4 institutions in 1 country.
Funding
No grant is acknowledged in the PubMed record.
Abstract
introductionPhosphatidylinositol 3-kinases (PI3Ks) overexpression can elicit cellular homeostatic dysregulation, which further contributes to tumorigenesis, with PI3Kα emerging as the most prevalent mutant isoform kinase among PI3Ks. Therefore, selective inhibitors targeting PI3Kα have attracted considerable interest in recent years. Molecular hybridization, with the advantage of simplified pharmacokinetics and drug-drug interactions, emerged as one of the important avenues for discovering potential drugs.
objectivesThis study aimed to construct PI3Kα inhibitors by hybridization and investigate their antitumor activity and mechanism.
methods26 quinazoline-2-indolinone derivatives were obtained by molecular hybridization, and their structure-activity relationship was analyzed by MTT, in vitro kinase activity and molecular docking. The biological evaluation of compound 8 was performed by transwell, flow cytometry, laser scanning confocal microscopy, Western blot, CTESA and immunohistochemistry.
resultsHere, we employed molecular hybridization methods to construct a series of quinazoline-2-indolinone derivatives as PI3Kα selective inhibitors. Encouragingly, representative compound 8 exhibited a PI3Kα enzymatic IC
conclusionsThis study presented a new avenue for the development of PI3Kα inhibitors and provided a solid foundation for novel QHIDs as potential future therapies for the treatment of NSCLC.
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