TY - JOUR
T1 - 1,4,5,6-Tetrahydropyrrolo[3,4-c]pyrazoles
T2 - Identification of a potent aurora kinase inhibitor with a favorable antitumor kinase inhibition profile
AU - Fancelli, Daniele
AU - Moll, Jürgen
AU - Varasi, Mario
AU - Bravo, Rodrigo
AU - Artico, Roberta
AU - Berta, Daniela
AU - Bindi, Simona
AU - Cameron, Alexander
AU - Candiani, Ilaria
AU - Cappella, Paolo
AU - Carpinelli, Patrizia
AU - Croci, Walter
AU - Forte, Barbara
AU - Giorgini, Maria Laura
AU - Klapwijk, Jan
AU - Marsiglio, Aurelio
AU - Pesenti, Enrico
AU - Rocchetti, Maurizio
AU - Roletto, Fulvia
AU - Severino, Dino
AU - Soncini, Chiara
AU - Storici, Paola
AU - Tonani, Roberto
AU - Zugnoni, Paola
AU - Vianello, Paola
PY - 2006/11/30
Y1 - 2006/11/30
N2 - 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.
AB - 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.
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U2 - 10.1021/jm060897w
DO - 10.1021/jm060897w
M3 - Article
C2 - 17125279
AN - SCOPUS:33845367377
VL - 49
SP - 7247
EP - 7251
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 24
ER -