4-（唑基苯基）-酞嗪-1-胺：血管内皮生长因子受体I和II的新型抑制剂。
4-(Azolylphenyl)-phthalazin-1-amines: Novel inhibitors of VEGF receptors I and II.
作者信息
Kiselyov Alexander S, Semenov Victor V, Milligan Daniel
机构信息
Chemical Diversity, Inc., 11558 Sorrento Valley Road, San Diego, CA 92121, USA.
出版信息
Chem Biol Drug Des. 2006 Dec;68(6):308-13. doi: 10.1111/j.1747-0285.2006.00456.x.
Novel potent derivatives of phthalazine are described as ATP-competitive inhibitors of vascular endothelial growth factor receptors I and II (VEGFR-1/2). A number of compounds display VEGFR-2 inhibitory activity reaching that of Vatalanib 3 (IC50 < 100 nm) in an HTRF enzymatic assay. Several derivatives also show good potential for the development as VEGFR-2 specific inhibitors showing 15-20-fold selectivity over VEGFR-1.
酞嗪的新型强效衍生物被描述为血管内皮生长因子受体I和II（VEGFR-1/2）的ATP竞争性抑制剂。在HTRF酶促试验中，许多化合物表现出VEGFR-2抑制活性，达到了凡他尼布3的抑制活性水平（IC50 < 100 nm）。几种衍生物还显示出作为VEGFR-2特异性抑制剂开发的良好潜力，对VEGFR-1具有15至20倍的选择性。
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