Discovery of novel anti-angiogenesis agents. Part 9: Multiplex inhibitors suppressing compensatory activations of RTKs.
Discovery of novel anti-angiogenesis agents. Part 9: Multiplex inhibitors suppressing compensatory activations of RTKs.
复制标题
新型抗血管生成剂的发现。
DOI：
10.1016/j.ejmech.2018.12.067
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发表时间：
2019-02
影响因子：
6.7
通讯作者：
Qinhua Chen
中科院分区：
文献类型：
--
作者：
Yuanyuan Shan;Ru Si;Jin Wang;Qingqing Zhang;Huaxin Zhou;Jie Song;Jie Zhang;Qinhua Chen
Aberrant angiogenesis is a hallmark of various diseases including cancers. VEGFR-2 inhibitors have been utilized as anti-angiogenic agents for several years. However, compensatory activation of various receptor tyrosine kinases (RTK) could induce the occurrence of resistance. We previously reported a series of multi-target inhibitors of VEGFR-2, Tie-2, and EphB4 as anti-angiogenic agents. These inhibitors might be a promising strategy to overcome the resistance induced by compensatory activation. In order to expand the structural diversity of these multiple RTK inhibitors, we described herein the design, synthesis, and evaluation of a novel class of triplet VEGFR-2/TIE-2/EphB4 inhibitors. The biological evaluation indicated that five compounds (6b, 6d, 6e, 7e, and7g) exhibited simultaneous VEGFR-2/Tie-2/EphB4 inhibitory activities with IC50values less than 50 nM.
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影响因子：
6.7
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发现多靶点受体酪氨酸激酶抑制剂作为新型抗血管生成剂
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