Evaluation of new 5-benzylidenethiazolidin-2,4-dione derivatives linked to nitric oxide donor oxime moiety as VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative assessment and studies.
1/5 보강
[AIM] Approaching VEGFR-2 blockers, two novel series of 5-benzylidenethiazolidine-2,4-dione and were synthesized.
APA
Abd El-Hameed AM, Ahmed NM, et al. (2026). Evaluation of new 5-benzylidenethiazolidin-2,4-dione derivatives linked to nitric oxide donor oxime moiety as VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative assessment and studies.. Future medicinal chemistry, 18(8), 943-960. https://doi.org/10.1080/17568919.2026.2642678
MLA
Abd El-Hameed AM, et al.. "Evaluation of new 5-benzylidenethiazolidin-2,4-dione derivatives linked to nitric oxide donor oxime moiety as VEGFR-2 inhibitors and apoptosis inducers: design, synthesis, anti-proliferative assessment and studies.." Future medicinal chemistry, vol. 18, no. 8, 2026, pp. 943-960.
PMID
41837691 ↗
Abstract 한글 요약
[AIM] Approaching VEGFR-2 blockers, two novel series of 5-benzylidenethiazolidine-2,4-dione and were synthesized.
[METHODS] Screening against and cancer cell lines.
[RESULTS] Derivatives and employed cytotoxicity against (22.75% to 55.30%) (Doxorubicin = 87.6%). Compound presented IC of 90.70 µM for (Doxorubicin = 32.36 µM). Concerning HCT-116 cell line, compounds 17d, 17e, and 17f haunted % inhibition (59.15% to 83.76%) (Doxorubicin = 96.8%). Besides, 17d, 17e, and 17f exhibited IC of 36.11, 54.50, and 67.22 µM, respectively (Doxorubicin = 21.27 µM). Also, compounds and disclosed safety outlines alongside normal cell IC (109.5 to 165 µM) (Doxorubicin = 38.51 µM). Compound arrested cell cycle at G2/M stage. Compounds released NO potentiating anti-cancer activity. , and inhibit VEGFR-2 (IC of 50.0 nM, 23.0 nM, and 111.0 nM, respectively) and sunitinib (84.0 nM). Western blot results displayed compound notable inhibition of the VEGFR-2/Akt/ERK axis. Docking studies revealed derivatives 17d-f docking score of -8.3 to -8.9 Kcal/Mol comparable to sunitinib and sorafenib.
[CONCLUSION] The present work flags the approach for advanced expansion of powerful nitric oxide donor offshoots as VEGFR-2 inhibitors.
[METHODS] Screening against and cancer cell lines.
[RESULTS] Derivatives and employed cytotoxicity against (22.75% to 55.30%) (Doxorubicin = 87.6%). Compound presented IC of 90.70 µM for (Doxorubicin = 32.36 µM). Concerning HCT-116 cell line, compounds 17d, 17e, and 17f haunted % inhibition (59.15% to 83.76%) (Doxorubicin = 96.8%). Besides, 17d, 17e, and 17f exhibited IC of 36.11, 54.50, and 67.22 µM, respectively (Doxorubicin = 21.27 µM). Also, compounds and disclosed safety outlines alongside normal cell IC (109.5 to 165 µM) (Doxorubicin = 38.51 µM). Compound arrested cell cycle at G2/M stage. Compounds released NO potentiating anti-cancer activity. , and inhibit VEGFR-2 (IC of 50.0 nM, 23.0 nM, and 111.0 nM, respectively) and sunitinib (84.0 nM). Western blot results displayed compound notable inhibition of the VEGFR-2/Akt/ERK axis. Docking studies revealed derivatives 17d-f docking score of -8.3 to -8.9 Kcal/Mol comparable to sunitinib and sorafenib.
[CONCLUSION] The present work flags the approach for advanced expansion of powerful nitric oxide donor offshoots as VEGFR-2 inhibitors.
🏷️ 키워드 / MeSH 📖 같은 키워드 OA만
- Humans
- Vascular Endothelial Growth Factor Receptor-2
- Cell Proliferation
- Apoptosis
- Antineoplastic Agents
- Drug Design
- Structure-Activity Relationship
- Molecular Docking Simulation
- Drug Screening Assays
- Antitumor
- Nitric Oxide Donors
- Protein Kinase Inhibitors
- Molecular Structure
- Dose-Response Relationship
- Drug
- MCF-7 Cells
- VEGFR-2 inhibitors
- breast cancer
- colon cancer
- nitric oxide donor
- thiazoldin-2
- 4-dione
🏷️ 같은 키워드 · 무료전문 — 이 논문 MeSH/keyword 기반
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