Design, synthesis, and anti-tumor evaluation of indolin-2-one derivatives based on 3D-QSAR.
2/5 보강
OpenAlex 토픽 ·
Protein Kinase Regulation and GTPase Signaling
Cytokine Signaling Pathways and Interactions
Protein Tyrosine Phosphatases
Tropomyosin receptor kinase (TRK) plays a critical role in tumorigenesis, and its aberrant activation is strongly implicated in cancer progression and metastasis.
APA
Xingdan Wang, Liying Zhang, et al. (2026). Design, synthesis, and anti-tumor evaluation of indolin-2-one derivatives based on 3D-QSAR.. Bioorganic & medicinal chemistry letters, 136, 130618. https://doi.org/10.1016/j.bmcl.2026.130618
MLA
Xingdan Wang, et al.. "Design, synthesis, and anti-tumor evaluation of indolin-2-one derivatives based on 3D-QSAR.." Bioorganic & medicinal chemistry letters, vol. 136, 2026, pp. 130618.
PMID
41825650 ↗
Abstract 한글 요약
Tropomyosin receptor kinase (TRK) plays a critical role in tumorigenesis, and its aberrant activation is strongly implicated in cancer progression and metastasis. In this study, a series of novel indoline-2-one derivatives were designed and synthesized using a 3D-QSAR-guided approach targeting TRK. The antitumor potential of these compounds was evaluated through a panel of in vitro bioassays. Several derivatives were found to reduce TRK phosphorylation levels in a cellular context and exhibited pronounced anti-proliferative and anti-migratory effects. Among them, compound IIIc demonstrated potent activity against HepG2 hepatocellular carcinoma cells, with an IC₅₀ value of 2.06 μM. Furthermore, ELISA-based phosphorylation assays revealed that treatment with compound IIIc resulted in decrease in TRK phosphorylation, yielding an IC₅₀ of 0.19 μM, highlighting its therapeutic promise. Collectively, this study provides experimental evidence and a structural basis for the development of lead compounds capable of modulating TRK signaling in cancer therapy.
🏷️ 키워드 / MeSH 📖 같은 키워드 OA만
- Humans
- Antineoplastic Agents
- Quantitative Structure-Activity Relationship
- Drug Design
- Indoles
- Drug Screening Assays
- Antitumor
- Cell Proliferation
- Hep G2 Cells
- Phosphorylation
- Molecular Structure
- Protein Kinase Inhibitors
- Dose-Response Relationship
- Drug
- Receptor
- trkA
- Cell Movement
- Cell Line
- Tumor
- 3D-QSAR
- Antitumor activity
- Indolin-2-one derivatives
- Molecular docking
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