Design, synthesis and biological evaluation of biphenylurea derivatives as VEGFR-2 kinase inhibitors（Ⅱ）

Inhibition of VEGFR-2 signaling pathway is one of the most promising approaches for the treatment of cancer. In this paper, we reported the design, synthesis, and biological evaluation of a series of biphenylurea derivatives as VEGFR-2 inhibitors. Among these compounds, 39 exhibited potent inhibitor...

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Published in中国化学快报：英文版 no. 2; pp. 200 - 204
Main Author Guo-Rui Gao Meng-Yuan Li Yong-Cong Lv Su-Fen Cao Lin-Jiang Tong Li-Xin Wei Jian Ding Hua Xie Wen-Hu Duan
Format Journal Article
LanguageEnglish
Published 2016
Subjects
受体
合成
抑制活性
生物学评价
衍生物
设计
酶抑制剂
鸡胚绒毛尿囊膜
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Summary:Inhibition of VEGFR-2 signaling pathway is one of the most promising approaches for the treatment of cancer. In this paper, we reported the design, synthesis, and biological evaluation of a series of biphenylurea derivatives as VEGFR-2 inhibitors. Among these compounds, 39 exhibited potent inhibitory activity against VEGFR-2 both in vitro and in vivo. The antiangiogenesis activity of 39 was further confirmed by both tube formation assay and chick chorioallantoic membrane assay.
Bibliography:11-2710/O6
Inhibition of VEGFR-2 signaling pathway is one of the most promising approaches for the treatment of cancer. In this paper, we reported the design, synthesis, and biological evaluation of a series of biphenylurea derivatives as VEGFR-2 inhibitors. Among these compounds, 39 exhibited potent inhibitory activity against VEGFR-2 both in vitro and in vivo. The antiangiogenesis activity of 39 was further confirmed by both tube formation assay and chick chorioallantoic membrane assay.
Angiogenesis; Kinase ;Inhibitor ;VEGFR-2
ISSN:1001-8417
1878-5964