1. Thieno[3,2-c]pyrazoles: A novel class of Aurora inhibitors with favorable antitumor activity
- Author
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Bindi, Simona, Fancelli, Daniele, Alli, Cristina, Berta, Daniela, Bertrand, Jay A., Cameron, Alexander D., Cappella, Paolo, Carpinelli, Patrizia, Cervi, Giovanni, Croci, Valter, D’Anello, Matteo, Forte, Barbara, Laura Giorgini, M., Marsiglio, Aurelio, Moll, Juergen, Pesenti, Enrico, Pittalà, Valeria, Pulici, Maurizio, Riccardi-Sirtori, Federico, and Roletto, Fulvia
- Subjects
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PYRAZOLES , *ANTINEOPLASTIC agents , *PROTEIN kinases , *STRUCTURE-activity relationship in pharmacology , *CELL lines , *PHARMACOKINETICS , *CELL cycle - Abstract
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. [ABSTRACT FROM AUTHOR]
- Published
- 2010
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