Synthesis and anti-angiogenetic activity evaluation of N-(3-aryl acryloyl)aminosaccharide derivatives

• Nineteen N-(3-aryl acryloyl)aminosaccharide derivatives were synthesized.
• Their anti-angiogenetic activity was evaluated by MTT assay and CAM assay.
• Compound 10s and topotecan had comparable effects on anti-angiogenesis.
• Electron-withdrawing group and disaccharide structure are beneficial.

In order to find novel potent inhibitors for signal pathways of FGF/FGFR, nineteen N-(3-aryl acryloyl)aminosaccharide derivatives were designed and synthesized based on the binding sites of FGF and oligosaccharides of heparin. Their structures were confirmed by IR, 1H NMR, 13C NMR, MS and elemental analysis. The nineteen target compounds were evaluated for biological activity against HUVEC cell. In vitro assays showed that compound 10s (IC50 = 5.3 μM) exhibited comparable inhibitory effects on endothelial cell growth with topotecan (IC50 = 2.7 μM). Compound 10s (10 μg/egg) also showed obvious anti-angiogenetic activity in the in vivo chicken chorio allantoic membrane (CAM) assay, and the potency was similar to topotecan (10 μg/egg).

Figure optionsDownload as PowerPoint slide