# Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGF

**Authors:** Shengying Lin, Maggie Suisui Guo, Roy Wai-Lun Tang, Yutong Ye, Jiahui Wu, Yuen Man Ho, Ran Duan, Ka Wing Leung, Tina Ting-Xia Dong, Karl Wah-Keung Tsim

PMC · DOI: 10.3390/molecules30112345 · Molecules · 2025-05-27

## TL;DR

A new resveratrol-like compound called RE-1 was developed and shown to strongly inhibit VEGF, a protein linked to diseases like cancer and macular degeneration.

## Contribution

A novel resveratrol-type analogue, RE-1, was synthesized and shown to have superior VEGF inhibitory activity compared to resveratrol.

## Key findings

- RE-1 exhibits robust inhibitory activity against VEGF and its downstream signaling pathways.
- RE-1 outperforms resveratrol in suppressing VEGF-mediated bioactivities.
- RE-1 shows potential for pharmacological development in treating VEGF-related diseases.

## Abstract

Vascular endothelial growth factor (VEGF), also known as VEGF-A, has been reported to mediate various diseases, including cancer and wet age-related macular degeneration (wAMD). Despite the fact that VEGF inhibitors are commercially available and appear to be effective in clinical applications, adverse effects have been caused by these treatments. There is an unmet need for developing novel VEGF-targeted treatments against these diseases. Resveratrol, a phytochemical derived from fruits and vegetables, has shown promising potency in suppressing VEGF-mediated bioactivities through a series of in vitro and in vivo testing models. Herein, we report that RE-1, a synthetic resveratrol-type analog, displays robust inhibitory activities against VEGF and its downstream signaling pathways, surpassing its parental molecule, resveratrol. In addition, the drug capabilities of RE-1 were evaluated. As a newly synthesized chemical, RE-1 could be considered for subsequent pharmacological development targeting VEGF-related diseases.

## Linked entities

- **Genes:** VEGFA (vascular endothelial growth factor A) [NCBI Gene 7422], VEGFA (vascular endothelial growth factor A) [NCBI Gene 7422]
- **Chemicals:** Resveratrol (PubChem CID 5056), RE-1 (PubChem CID 447188)
- **Diseases:** cancer (MONDO:0004992)

## Full-text entities

- **Genes:** VEGFA (vascular endothelial growth factor A) [NCBI Gene 7422] {aka L-VEGF, MVCD1, VEGF, VPF}
- **Diseases:** cancer (MESH:D009369), age-related macular degeneration (MESH:D008268), wAMD (MESH:D057135)
- **Chemicals:** Resveratrol (MESH:D000077185), RE-1 (-)

## Full text

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## Figures

8 figures with captions in the complete paper: https://tomesphere.com/paper/PMC12155980/full.md

## References

38 references — full list in the complete paper: https://tomesphere.com/paper/PMC12155980/full.md

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Source: https://tomesphere.com/paper/PMC12155980