Synthesis and Evaluation of Vascular Endothelial Growth Factor Receptor-2 Inhibitory Activity of 6,7-Dimethoxycinnoline Derivatives

Author(s): Xingjun Yao, Hongfa Yang, Yanhui Wan, Li Bie, Xinrui Liu, Zhonghui Liu

Journal Name: Letters in Drug Design & Discovery

Volume 10 , Issue 10 , 2013

Become EABM
Become Reviewer


A series of 6, 7-Dimethoxycinnoline derivatives were prepared as vascular endothelial growth factor receptor 2 (VEGFR-2) inhibitors and their activity to inhibit VEGFR-2 and epidermal growth factor receptor (EGFR) were evaluated. The structure-activity studies on compounds screening led to the discovery of a novel series of potent and selective VEGFR-2 inhibitors. Compound 6-(6,7-dimethoxycinnolin -4-yloxy)-N-(4-chlorophenyl)naphthalene-1-carboxamide 7a showed potent VEGFR-2 inhibitory activity and good selectivity against EGFR.

Keywords: Inhibit EGFR Activity, Inhibit VEGFR-2 Activity, 6, 7-Dimethoxycinnoline Derivatives, Anticancer, Synthesis.

Rights & PermissionsPrintExport Cite as

Article Details

Year: 2013
Published on: 24 October, 2013
Page: [984 - 988]
Pages: 5
DOI: 10.2174/15701808113109990027
Price: $65

Article Metrics

PDF: 5