Design and synthesis of thiadiazoles as anticancer, apoptotic, and VEGFR-2 inhibitors DOI
Walid E. Elgammal, Hazem Elkady, Mohammed A. Dahab

et al.

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 13

Published: April 8, 2025

Vascular endothelial growth factor receptor (VEGFR-2) inhibitors are critical in cancer therapy due to their role suppressing tumor angiogenesis. Herein, we report a new series of thiadiazole-based derivatives as potential VEGFR-2 with promising anticancer activity. The synthesized compounds were evaluated for anti-proliferative activity against human cell lines (HCT-116, MCF-7, and HepG-2), WI-38 normal cells. Sorafenib was used reference drug. inhibitory determined, followed by cycle analysis, apoptosis assays, Q-RT-PCR wound-healing assays. In silico molecular docking conducted explore binding interactions. Among the tested compounds, 13b exhibited potent (IC50: 3.98-11.81 µM) strong inhibition 41.51 nM), surpassing sorafenib 53.32 nM). Cell analysis revealed that induced G2/M phase arrest MCF-7 Apoptosis levels increased from 2% 52%, accompanied > 12-fold rise Bax/Bcl-2 ratio activation caspase-8/9. Additionally, significantly suppressed migration, only 5.28% wound closure. studies confirmed its Thiadiazole-based derivatives, particularly compound 13b, exhibit inhibition, effects, induction, anti-migratory activity, supporting agents.

Language: Английский

Anti-breast cancer potential of thieno-pyrimidine derivatives as VEGFR-2 inhibitors DOI
Aisha A. Alsfouk, Maged Mohammed Saleh Al Ward,

Mustafa A. Al-Qadhi

et al.

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 16

Published: March 17, 2025

Background Thieno-pyrimidine derivatives have emerged as promising candidates for VEGFR-2 inhibition. This study aimed to design, synthesize, and evaluate novel thieno-pyrimidine their anti-cancer potential.

Language: Английский

Citations

0
Design and synthesis of thiadiazoles as anticancer, apoptotic, and VEGFR-2 inhibitors DOI
Walid E. Elgammal, Hazem Elkady, Mohammed A. Dahab

et al.

Future Medicinal Chemistry, Journal Year: 2025, Volume and Issue: unknown, P. 1 - 13

Published: April 8, 2025

Vascular endothelial growth factor receptor (VEGFR-2) inhibitors are critical in cancer therapy due to their role suppressing tumor angiogenesis. Herein, we report a new series of thiadiazole-based derivatives as potential VEGFR-2 with promising anticancer activity. The synthesized compounds were evaluated for anti-proliferative activity against human cell lines (HCT-116, MCF-7, and HepG-2), WI-38 normal cells. Sorafenib was used reference drug. inhibitory determined, followed by cycle analysis, apoptosis assays, Q-RT-PCR wound-healing assays. In silico molecular docking conducted explore binding interactions. Among the tested compounds, 13b exhibited potent (IC50: 3.98-11.81 µM) strong inhibition 41.51 nM), surpassing sorafenib 53.32 nM). Cell analysis revealed that induced G2/M phase arrest MCF-7 Apoptosis levels increased from 2% 52%, accompanied > 12-fold rise Bax/Bcl-2 ratio activation caspase-8/9. Additionally, significantly suppressed migration, only 5.28% wound closure. studies confirmed its Thiadiazole-based derivatives, particularly compound 13b, exhibit inhibition, effects, induction, anti-migratory activity, supporting agents.

Language: Английский

Citations

0