کد مقاله | کد نشریه | سال انتشار | مقاله انگلیسی | نسخه تمام متن |
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1359904 | 981419 | 2010 | 8 صفحه PDF | دانلود رایگان |
![عکس صفحه اول مقاله: Thieno[3,2-c]pyrazoles: A novel class of Aurora inhibitors with favorable antitumor activity Thieno[3,2-c]pyrazoles: A novel class of Aurora inhibitors with favorable antitumor activity](/preview/png/1359904.png)
A novel series of 3-amino-1H-thieno[3,2-c]pyrazole derivatives demonstrating high potency in inhibiting Aurora kinases was developed. Here we describe the synthesis and a preliminary structure–activity relationship, which led to the discovery of a representative compound (38), which showed low nanomolar inhibitory activity in the anti-proliferation assay and was able to block the cell cycle in HCT-116 cell line. This compound demonstrated favorable pharmacokinetic properties and good efficacy in the HL-60 xenograft tumor model.
In this paper we report on the optimization of the thieno[3,2-c]pyrazole series as inhibitors of the Aurora kinases to give a promising lead compound endowed with high potency in in vitro assays and active in vivo in the HL-60 xenograft tumor model.Figure optionsDownload as PowerPoint slide
Journal: Bioorganic & Medicinal Chemistry - Volume 18, Issue 19, 1 October 2010, Pages 7113–7120