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Lookup NU author(s): Professor Steve Wedge
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A new class of 1-acetanilide-4-aminopyrazole-substituted quinazoline Aurora kinase inhibitors has been discovered possessing highly potent cellular activity. Continuous infusion into athymic mice bearing SW620 tumors of the soluble phosphate derivative 2 led to dose-proportional exposure of the des-phosphate compound 8 with a high-unbound fraction. The combination of potent cell activity and high free-drug exposure led to pharmacodynamic changes in the tumor at low doses, indicative of Aurora B-kinase inhibition and a reduction in tumor volume.
Author(s): Foote KM, Mortlock AA, Heron NM, Jung FH, Hill GB, Pasquet G, Brady MC, Green S, Heaton SP, Kearney S, Keen NJ, Odedra R, Wedge SR, Wilkinson RW
Publication type: Article
Publication status: Published
Journal: Bioorganic & Medicinal Chemistry Letters
Year: 2008
Volume: 18
Issue: 6
Pages: 1904-1909
ISSN (print): 0960-894X
ISSN (electronic): 1464-3405
Publisher: Elsevier
URL: http://dx.doi.org/10.1016/j.bmcl.2008.02.002
DOI: 10.1016/j.bmcl.2008.02.002
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