AI Article Synopsis
- A new series of compounds called 4-(benzofuran-6-yloxy)quinazoline derivatives were created as dual inhibitors targeting VEGFR-2 and HDAC, inspired by existing drugs fruquintinib and vorinostat.
- Among these compounds, compound 13 showed strong inhibitory effects on VEGFR-2 and HDAC1, with impressive antiproliferative activity against various cancer cell lines like MCF-7 and HeLa.
- Compound 13 slowed down cell growth during specific cell cycle phases and caused significant cell death in HeLa cells, while also demonstrating anti-angiogenic effects, making it a promising candidate for further cancer treatment research.
Article Abstract
Herein, a series of 4-(benzofuran-6-yloxy)quinazoline derivatives as VEGFR-2/HDAC dual inhibitors were designed and synthesized based on fruquintinib and vorinostat. Among them, compound 13 exhibited potent inhibitory activity against VEGFR-2 and HDAC1 with IC values of 57.83 nM and 9.82 nM, and displayed moderate to significant antiproliferative activity against MCF-7, A549, HeLa and HUVEC. The cellular mechanism studies revealed that compound 13 arrested the cell cycle at the S and G2 phases, and induced significant apoptosis in HeLa cells. Tube formation assay in HUVECs demonstrated that 13 had a significant anti-angiogenic effect. Additionally, a molecular docking study supported the initial design strategy. These results highlighted that 13 was a valuable VEGFR-2/HDAC dual inhibitor and deserved further study for cancer therapy.
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Source |
|---|---|
| http://www.ncbi.nlm.nih.gov/pmc/articles/PMC10523135 | PMC |
| http://dx.doi.org/10.1039/d3ra05542f | DOI Listing |
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