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Artigo Revisado por pares
BIBTEX RIS

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

2011; Elsevier BV; Volume: 21; Issue: 18 Linguagem: Inglês

10.1016/j.bmcl.2011.07.027

ISSN

1464-3405

Autores

Sunny Abraham, Michael J. Hadd, Lan P. Tran, Troy Vickers, Janice A. Sindac, Zdravko V. Milanov, Mark W. Holladay, Shripad S. Bhagwat, Helen Hua, Julia M. Ford Pulido, Merryl Cramer, Dana Gitnick, Joyce James, Alan Dao, Barbara Belli, Robert C. Armstrong, Daniel K. Treiber, Gang Liu,

Tópico(s)

Cancer therapeutics and mechanisms

Resumo

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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