کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1254689 | 971386 | 2015 | 4 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I) Design, synthesis and biological evaluation of O-linked indoles as VEGFR-2 kinase inhibitors (I)](/preview/png/1254689.png)
Inhibition of VEGFR-2 signaling pathway has already become one of the most promising approaches for the treatment of cancer. In this study, we describe the design, synthesis, and biological evaluation of a series of O-linked indoles as potent inhibitors of VEGFR-2. Among these compounds, 18 showed significant anti-angiogenesis activities via VEGFR-2 in enzymatic proliferation assays, with IC50 value of 3.8 nmol/L. Kinase selectivity profiling revealed that 18 was a multitargeted inhibitor, and it also exhibited good potency against VEGFR-1, PDGFR-α and β.
In an effort to discover potent VEGFR-2 inhibitors, a series of 2,4 or 4,6-disubstituted O-linked indoles derivatives were designed and synthesized. The structural activity relationships led to identification of a potential VEGFR-2 inhibitor compound 18.Figure optionsDownload as PowerPoint slide
Journal: Chinese Chemical Letters - Volume 26, Issue 9, September 2015, Pages 1165–1168