2. Academic Validation
  3. Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors

Novel series of pyrrolotriazine analogs as highly potent pan-Aurora kinase inhibitors

  • Bioorg Med Chem Lett. 2011 Sep 15;21(18):5296-300. doi: 10.1016/j.bmcl.2011.07.027.
Sunny Abraham 1,  Michael J Hadd,  Lan Tran,  Troy Vickers,  Janice Sindac,  Zdravko V Milanov,  Mark W Holladay,  Shripad S Bhagwat,  Helen Hua,  Julia M Ford Pulido,  Merryl D Cramer,  Dana Gitnick,  Joyce James,  Alan Dao,  Barbara Belli,  Robert C Armstrong,  Daniel K Treiber,  Gang Liu
Affiliations

Affiliation

  • 1 Department of Medicinal Chemistry, Ambit Biosciences Corporation, 4215 Sorrento Valley Boulevard, San Diego, CA 92121, United States.
PMID: 21802948 DOI: 10.1016/j.bmcl.2011.07.027
Abstract

The synthesis and SAR for a novel series of pyrrolotriazines as pan-Aurora kinase inhibitors are described. Optimization of the cyclopropane carboxamide terminus of lead compound 1 resulted in analogs with high cellular activity and improved rat PK profiles. Notably, compound 17l demonstrated tumor growth inhibition in a mouse xenograft model.

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