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Synthesis and SAR of 1-acetanilide-4-aminopyrazole-substituted quinazolines: selective inhibitors of Aurora B kinase with potent anti-tumor activity

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.

Publication metadata

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


DOI: 10.1016/j.bmcl.2008.02.002


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