Letters in Drug Design & Discovery

G. Perry
University of Texas
San Antonio, TX
USA
Email: lddd@benthamscience.org

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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.

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.

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

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Article Details

VOLUME: 10
ISSUE: 10
Year: 2013
Page: [984 - 988]
Pages: 5
DOI: 10.2174/15701808113109990027
Price: $58