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1,4,5,6-Tetrahydropyrrolo[3,4- c ]pyrazoles: Identification of a Potent Aurora Kinase Inhibitor with a Favorable Antitumor Kinase Inhibition Profile

2006; American Chemical Society; Volume: 49; Issue: 24 Linguagem: Inglês

10.1021/jm060897w

1520-4804

Daniele Fancelli, Jürgen Moll, Mario Varasi, Rodrigo Bravo, Roberta Artico, Daniela Berta, Simona Bindi, Alexander D. Cameron, Ilaria Candiani, Paolo Cappella, Patrizia Carpinelli, Walter Croci, Barbara Forte, Maria Laura Giorgini, Jan Klapwijk, Aurelio Marsiglio, Enrico Pesenti, Maurizio Rocchetti, Fulvia Roletto, D. Severino, Chiara Soncini, Paola Storici, R. Tonani, Paola Zugnoni, Paola Vianello,

Neuroblastoma Research and Treatments

The optimization of a series of 5-phenylacetyl 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole derivatives toward the inhibition of Aurora kinases led to the identification of compound 9d. This is a potent inhibitor of Aurora kinases that also shows low nanomolar potency against additional anticancer kinase targets. Based on its high antiproliferative activity on different cancer cell lines, favorable chemico-physical and pharmacokinetic properties, and high efficacy in in vivo tumor models, compound 9d was ultimately selected for further development.