Citation: 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. Design, synthesis and biological evaluation of biphenylurea derivatives as VEGFR-2 kinase inhibitors (Ⅱ)[J]. Chinese Chemical Letters, ;2016, 27(02): 200-204. doi: 10.1016/j.cclet.2015.10.004 shu

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

Guo-Rui Gao ^a ,
Meng-Yuan Li ^b,d ,
Yong-Cong Lv ^c ,
Su-Fen Cao ^a ,
Lin-Jiang Tong ^b ,
Li-Xin Wei ^d ,
Jian Ding ^b ,
Hua Xie ^b ,
Wen-Hu Duan ^a,c,,

a.
a. School of Pharmacy, East China University of Science & Technology, Shanghai 200237, China;
b.
b. Division of Anti-tumor Pharmacology, State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;
c.
c. Department of Medicinal Chemistry, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai 201203, China;
d.
d. Pharmacology and Safety Evaluation Key Laboratory of Tibetan Medicine in Qinghai Province, Northwest Institute of Plateau Biology, Chinese Academy of Sciences, Xining 810008, China

Corresponding author: Wen-Hu Duan,
Received Date: 23 June 2015
Available Online: 12 July 2015
Fund Project: We thank the National Natural Science Foundation of China (Nos. 81273365, 81173080, 81321092) (Nos. 81273365, 81173080, 81321092) Chinese National Programs for High Technology Research and Development (No. 2012AA020302) (Nos. 2012ZX09103101-024, 2014ZX09304002-008-001)

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
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