99138-83-7Relevant academic research and scientific papers
A novel 2-aminobenzimidazole-based compound Jzu 17 exhibits anti-angiogenesis effects by targeting VEGFR-2 signalling
Lien, Jin-Cherng,Chung, Chi-Li,Huang, Tur-Fu,Chang, Tsung-Chia,Chen, Kuan-Chung,Gao, Ging-Yan,Hsu, Ming-Jen,Huang, Shiu-Wen
supporting information, p. 4034 - 4049 (2019/11/02)
Background and Purpose: Recent development in drug discovery have shown benzimidazole to be an important pharmacophore,. Benzimidazole derivatives exhibit broad-spectrum pharmacological properties including anti-microbial, anti-diabetic and anti-tumour activity. However, whether benzimidazole derivatives are effective in suppressing angiogenesis and its underlying mechanisms remain incompletely understood. In this study, we aim to characterize the anti-angiogenic mechanisms of a novel 2-aminobenzimidazole-based compound, Jzu 17, in an effort to develop novel angiogenesis inhibitor. Experimental Approach: Effects of Jzu 17 on endothelial cell proliferation, migration, invasion, and activation of signalling molecules induced by VEGF-A, were analysed by immunoblotting, MTT, BrdU, migration, and invasion assays. We performed tube formation assay, aorta ring sprouting assay, matrigel plug assay, and a mouse model of metastasis to evaluate ex vivo and in vivo anti-angiogenic effects of Jzu 17. Key Results: Jzu 17 inhibited VEGF-A-induced cell proliferation, migration, invasion, and endothelial tube formation of HUVECs. Jzu 17 suppressed VEGF-A-induced microvessel sprouting ex vivo and attenuated VEGF-A- or tumour cell-induced neovascularization in vivo. Jzu 17 also reduced B16F10 melanoma lung metastasis. In addition, Jzu 17 inhibited the phosphorylation of VEGFR-2 and its downstream signalling molecules in VEGF-A-stimulated HUVECs. Results from computer modelling further showed that Jzu 17 binds to VEGFR-2 with high affinity. Conclusions and Implications: Jzu 17 may inhibit endothelial remodelling and suppress angiogenesis through targeting VEGF-A-VEGFR-2 signalling. These results also suggest Jzu 17 as a potential lead compound and warrant the clinical development of similar agents in the treatment of cancer and angiogenesis-related diseases.
Synthesis, Antibacterial, and Antifungal Activities of Some New Benzimidazoles
Vlaovic, Djordje,Canadanovic-Brunet, Jasna,Balaz, Jelica,Juranic, Ivan,Djokovic, Dejan,Mackenzie, Kenneth
, p. 199 - 206 (2007/10/02)
1,2-Diaminobenzimidazoles 2 were synthesized by N-amination of 2-aminobenzimidazoles 1 with hydroxylamine-O-sulphonic acid.Substituted 1-alkyl and 1-alkylarylbenzimidazoles 3 were prepared from various benzimidazoles by alkylating with the corresponding a
Anti-allergic five membered heterocyclic ring containing N-(bicyclic heterocycyl)-4-piperidinamines
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, (2008/06/13)
Five membered heterocyclic ring containing N-(bicyclic heterocyclyl)-4-piperidinamines having histamine and serotonine antagonistic activity which compounds are useful agents in the treatment of allergic diseases.
