Development of novel furan-based VEGFR-2 inhibitors and apoptotic inducers for colorectal cancer.
1/5 보강
[AIMS] This study aimed to synthesize and evaluate novel furan derivatives as potential anticancer agents targeting colon cancer through VEGFR-2 inhibition and apoptosis induction.
APA
Elkaeed EB, Al Ward MMS, et al. (2025). Development of novel furan-based VEGFR-2 inhibitors and apoptotic inducers for colorectal cancer.. Future medicinal chemistry, 17(24), 2959-2973. https://doi.org/10.1080/17568919.2025.2587566
MLA
Elkaeed EB, et al.. "Development of novel furan-based VEGFR-2 inhibitors and apoptotic inducers for colorectal cancer.." Future medicinal chemistry, vol. 17, no. 24, 2025, pp. 2959-2973.
PMID
41251277 ↗
Abstract 한글 요약
[AIMS] This study aimed to synthesize and evaluate novel furan derivatives as potential anticancer agents targeting colon cancer through VEGFR-2 inhibition and apoptosis induction.
[MATERIALS AND METHODS] The cytotoxic activity of the synthesized compounds was assessed against human fibroblast (HSF) and colon cancer cell lines (HCT-116, Caco-2, and HT-29) using the MTT assay. VEGFR-2 inhibitory activity was determined , and immunocytochemistry was employed to evaluate VEGFR-2 expression. Apoptosis, cell cycle arrest, and migration inhibition were analyzed in Caco-2 cells. Molecular docking, molecular dynamics (MD) simulations, Density Functional Theory (DFT), and ADMET analyses were conducted to assess binding affinity, stability, and safety profiles.
[RESULTS] Compound exhibited potent cytotoxicity against HT-29 (IC = 22.39 μM) and strong VEGFR-2 inhibition (IC = 0.28 ± 0.42 μM), comparable to sorafenib. It suppressed VEGFR-2 expression, induced G2/M cell cycle arrest, and promoted early and late apoptosis in 97% of treated Caco-2 cells. Upregulation of Bax and caspase-3, along with downregulation of Bcl-2, confirmed intrinsic apoptotic activation. Computational analyses supported compound 's stability and drug-likeness.
[CONCLUSIONS] Compound is a promising lead furan derivative with potent, selective anticancer activity against colon cancer VEGFR-2 inhibition and apoptosis induction. Further, evaluation is warranted.
[MATERIALS AND METHODS] The cytotoxic activity of the synthesized compounds was assessed against human fibroblast (HSF) and colon cancer cell lines (HCT-116, Caco-2, and HT-29) using the MTT assay. VEGFR-2 inhibitory activity was determined , and immunocytochemistry was employed to evaluate VEGFR-2 expression. Apoptosis, cell cycle arrest, and migration inhibition were analyzed in Caco-2 cells. Molecular docking, molecular dynamics (MD) simulations, Density Functional Theory (DFT), and ADMET analyses were conducted to assess binding affinity, stability, and safety profiles.
[RESULTS] Compound exhibited potent cytotoxicity against HT-29 (IC = 22.39 μM) and strong VEGFR-2 inhibition (IC = 0.28 ± 0.42 μM), comparable to sorafenib. It suppressed VEGFR-2 expression, induced G2/M cell cycle arrest, and promoted early and late apoptosis in 97% of treated Caco-2 cells. Upregulation of Bax and caspase-3, along with downregulation of Bcl-2, confirmed intrinsic apoptotic activation. Computational analyses supported compound 's stability and drug-likeness.
[CONCLUSIONS] Compound is a promising lead furan derivative with potent, selective anticancer activity against colon cancer VEGFR-2 inhibition and apoptosis induction. Further, evaluation is warranted.
🏷️ 키워드 / MeSH 📖 같은 키워드 OA만
- Humans
- Vascular Endothelial Growth Factor Receptor-2
- Apoptosis
- Furans
- Antineoplastic Agents
- Colorectal Neoplasms
- Drug Screening Assays
- Antitumor
- Molecular Docking Simulation
- Structure-Activity Relationship
- Cell Proliferation
- Protein Kinase Inhibitors
- Molecular Structure
- Dose-Response Relationship
- Drug
- Furan derivatives
- MD simulations
- VEGFR-2
- colon cancer
- design
- molecular docking
- synthesis
🏷️ 같은 키워드 · 무료전문 — 이 논문 MeSH/keyword 기반
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