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 efficacy in in vivo tumor models, compound 9d was ultimately selected for further development.
| Original language | English |
|---|---|
| Pages (from-to) | 7247-7251 |
| Number of pages | 5 |
| Journal | Journal of Medicinal Chemistry |
| Volume | 49 |
| Issue number | 24 |
| DOIs | |
| Publication status | Published - Nov 30 2006 |
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ASJC Scopus subject areas
- Organic Chemistry
Cite this
1,4,5,6-Tetrahydropyrrolo[3,4-c]pyrazoles : Identification of a potent aurora kinase inhibitor with a favorable antitumor kinase inhibition profile. / Fancelli, Daniele; Moll, Jürgen; 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.
In: Journal of Medicinal Chemistry, Vol. 49, No. 24, 30.11.2006, p. 7247-7251.Research output: Contribution to journal › Article
}
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.
UR - http://www.scopus.com/inward/record.url?scp=33845367377&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=33845367377&partnerID=8YFLogxK
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 -