Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGF
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, adve...
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MDPI AG
2025-05-01
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| Series: | Molecules |
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| Online Access: | https://www.mdpi.com/1420-3049/30/11/2345 |
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| author | 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 |
| author_facet | 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 |
| author_sort | Shengying Lin |
| collection | DOAJ |
| description | 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. |
| format | Article |
| id | doaj-art-22c5cf0f9fa64d71ba39f19ed3de1c8f |
| institution | DOAJ |
| issn | 1420-3049 |
| language | English |
| publishDate | 2025-05-01 |
| publisher | MDPI AG |
| record_format | Article |
| series | Molecules |
| spelling | doaj-art-22c5cf0f9fa64d71ba39f19ed3de1c8f2025-08-20T03:11:32ZengMDPI AGMolecules1420-30492025-05-013011234510.3390/molecules30112345Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGFShengying Lin0Maggie Suisui Guo1Roy Wai-Lun Tang2Yutong Ye3Jiahui Wu4Yuen Man Ho5Ran Duan6Ka Wing Leung7Tina Ting-Xia Dong8Karl Wah-Keung Tsim9Center for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaCenter for Chinese Medicine R & D, Division of Life Science, The Hong Kong University of Science and Technology, Clear Water Bay, Kowloon, Hong Kong, ChinaVascular 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.https://www.mdpi.com/1420-3049/30/11/2345VEGF inhibitorSAR studyresveratrol-type analogsangiogenesisage-related macular degenerationcancer |
| spellingShingle | 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 Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGF Molecules VEGF inhibitor SAR study resveratrol-type analogs angiogenesis age-related macular degeneration cancer |
| title | Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGF |
| title_full | Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGF |
| title_fullStr | Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGF |
| title_full_unstemmed | Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGF |
| title_short | Design, Synthesis, and Biological Evaluations of a Novel Resveratrol-Type Analogue Against VEGF |
| title_sort | design synthesis and biological evaluations of a novel resveratrol type analogue against vegf |
| topic | VEGF inhibitor SAR study resveratrol-type analogs angiogenesis age-related macular degeneration cancer |
| url | https://www.mdpi.com/1420-3049/30/11/2345 |
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