Design, Synthesis, Molecular Docking, and Anticancer Activity of Chalcone Derivatives as VEGFR-2 Inhibitors
Year: 2025
Type: article
Abstract: A series of 4-phenylurea chalcones (2a–2s) as VEGFR-2 inhibitors has been designed, synthesized, and evaluated for in vitro cytotoxic activity against K562, SiHa, and B16 cancer cells. Compared to sorafenib, the compounds exhibited strong cytotoxicity against K562, SiHa and B16 cells. Compounds 2r, 2o, and 2l exhibited remarkable cytotoxicity against K562, SiHa, and B16 cells, with IC50 values of 0.97 μM, 1.22 μM, and 1.39 μM, respectively. Moreover, compound 2l exhibited potent cytotoxicity against K562, SiHa, and B16, with IC50 values ranging from 1.25 μM to 1.39 μM. Compounds 2l and 2o also exhibited excellent inhibitory activity on VEGFR-2 kinase, with IC50 values of 0.42 ± 0.03 and 0.31 ± 0.02 μM, respectively. Molecular docking proved that the target compounds had strong binding interactions with VEGFR-2 proteins. Flow cytometry analysis showed that compound 2l induced apoptosis and arrested the cell cycle at the G1 and S phases.
Source: Molecules
Authors: Mingjun Yu, Xin Zhang, Hui Zhu, Xiaoqian Zhang
Institutions: Bozhou University, Hong Kong Baptist University
Language: English
Subfield: Organic Chemistry
Field: Chemistry
Domain: Physical Sciences
Open Access status: gold
Estimated APC paid: $3,258
Funder: Bozhou University
OpenAlex ID: W4416575165