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Thieno[3,2-c]pyrazoles: A novel class of Aurora inhibitors with favorable antitumor activity
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(2010) Thieno[3,2-c]pyrazoles: A novel class of Aurora inhibitors with favorable antitumor activity. Bioorganic & Medicinal Chemistry, Vol. 18 (No. 19). pp. 7113-7120. doi:10.1016/j.bmc.2010.07.048 ISSN 0968-0896.
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Official URL: http://dx.doi.org/10.1016/j.bmc.2010.07.048
Abstract
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.
| Item Type: | Journal Article | ||||
|---|---|---|---|---|---|
| Divisions: | Faculty of Science, Engineering and Medicine > Science > Life Sciences (2010- ) | ||||
| Journal or Publication Title: | Bioorganic & Medicinal Chemistry | ||||
| Publisher: | Elsevier Science BV | ||||
| ISSN: | 0968-0896 | ||||
| Official Date: | 2010 | ||||
| Dates: |
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| Volume: | Vol. 18 | ||||
| Number: | No. 19 | ||||
| Page Range: | pp. 7113-7120 | ||||
| DOI: | 10.1016/j.bmc.2010.07.048 | ||||
| Status: | Peer Reviewed | ||||
| Publication Status: | Published | ||||
| Access rights to Published version: | Restricted or Subscription Access |
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