1, 4, 5, 6-tetrahydropyrrolo [3, 4-c] pyrazoles: identification of a potent Aurora kinase inhibitor with a favorable antitumor kinase inhibition profile

…, D Berta, S Bindi, A Cameron, I Candiani…

Index: Fancelli, Daniele; Moll, Juergen; Varasi, Mario; Bravo, Rodrigo; Artico, Roberta; Berta, Daniela; Bindi, Simona; Cameron, Alexander; Candiani, Ilaria; Cappella, Paolo; Carpinelli, Patrizia; Croci, Walter; Forte, Barbara; Giorgini, Maria Laura; Klapwijk, Jan; Marsiglio, Aurelio; Pesenti, Enrico; Rocchetti, Maurizio; Roletto, Fulvia; Severino, Dino; Soncini, Chiara; Storici, Paola; Tonani, Roberto; Zugnoni, Paola; Vianello, Paola Journal of Medicinal Chemistry, 2006 , vol. 49, # 24 p. 7247 - 7251

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Citation Number: 168

Abstract

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 ...