期刊
BIOORGANIC & MEDICINAL CHEMISTRY
卷 22, 期 1, 页码 277-284出版社
PERGAMON-ELSEVIER SCIENCE LTD
DOI: 10.1016/j.bmc.2013.11.027
关键词
Angiogenesis; VEGFR-2 inhibitor; Biphenyl scaffold; Urea moiety
资金
- National Natural Science Foundation (NNSF) of China [81302641, 81302737, 81230079]
- Fundamental Research Funds for the Central Universities
- Natural Science Basic Research Plan in Shaanxi Province of China [2011K15-05-02]
A series of novel biphenyl urea derivates were synthesized and investigated for their potential to inhibit vascular endothelial growth factor receptor-2 (VEGFR-2). In particular, A7, B3 and B4 displayed significant enzymatic inhibitory activities, with IC50 values of 4.06, 4.55 and 5.26 nM. Compound A7 exhibited potent antiproliferative activity on several cell lines. SAR study suggested that the introduction of methyl at ortho-position of the biphenyl urea and tertiary amine moiety could improve VEGFR-2 inhibitory activity and antitumor effects. Molecular docking indicated that the urea moiety formed four hydrogen bonds with DFG residue. These biphenyl ureas could serve as promising lead compounds for further optimization. (C) 2013 Elsevier Ltd. All rights reserved.
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