| Literature DB >> 20817473 |
Simona Bindi1, Daniele Fancelli, Cristina Alli, Daniela Berta, Jay A Bertrand, Alexander D Cameron, Paolo Cappella, Patrizia Carpinelli, Giovanni Cervi, Valter Croci, Matteo D'Anello, Barbara Forte, M Laura Giorgini, Aurelio Marsiglio, Juergen Moll, Enrico Pesenti, Valeria Pittalà, Maurizio Pulici, Federico Riccardi-Sirtori, Fulvia Roletto, Chiara Soncini, Paola Storici, Mario Varasi, Daniele Volpi, Paola Zugnoni, Paola Vianello.
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.Entities:
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Year: 2010 PMID： 20817473 DOI： 10.1016/j.bmc.2010.07.048
Source DB: PubMed Journal: Bioorg Med Chem ISSN： 0968-0896 Impact factor: 3.641