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- Title
A Macrocyclic Ruthenium(III) Complex Inhibits Angiogenesis with Down-Regulation of Vascular Endothelial Growth Factor Receptor-2 and Suppresses Tumor Growth In Vivo.
- Authors
Kwong, Wai‐Lun; Lam, Kar‐Yee; Lok, Chun‐Nam; Lai, Yau‐Tsz; Lee, Pui‐Yan; Che, Chi‐Ming
- Abstract
A macrocyclic ruthenium(III) complex [RuIII(N2O2)Cl2]Cl ( Ru-1) is reported as an inhibitor of angiogenesis and an anti-tumor compound. The complex is relatively non-cytotoxic towards endothelial and cancer cell lines in vitro, but specifically inhibited the processes of angiogenic endothelial cell tube formation and cancer cell invasion. Moreover, compared with known anti-cancer ruthenium complexes, Ru-1 is distinct in that it suppressed the expression of vascular endothelial growth factor receptor-2 (VEGFR2), and the associated downstream signaling that is crucial to tumor angiogenesis. In addition, in vivo studies showed that Ru-1 inhibited angiogenesis in a zebrafish model and suppressed tumor growth in nude mice bearing cancer xenografts.
- Subjects
MACROCYCLIC compounds; NEOVASCULARIZATION inhibitors; ENDOTHELIAL growth factors; TUMOR growth; CANCER cells; XENOGRAFTS
- Publication
Angewandte Chemie International Edition, 2016, Vol 55, Issue 43, p13524
- ISSN
1433-7851
- Publication type
Article
- DOI
10.1002/anie.201608094