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

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

Volume: 10 Issue: 10

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

Affiliation:

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

Abstract: 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.

Cite this article as:

Yao Xingjun, Yang Hongfa, Wan Yanhui, Bie Li, Liu Xinrui and Liu Zhonghui, Synthesis and Evaluation of Vascular Endothelial Growth Factor Receptor-2 Inhibitory Activity of 6,7-Dimethoxycinnoline Derivatives, Letters in Drug Design & Discovery 2013; 10 (10) . https://dx.doi.org/10.2174/15701808113109990027