TY - JOUR
T1 - Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition
AU - Fancelli, Daniele
AU - Berta, Daniela
AU - Bindi, Simona
AU - Cameron, Alexander
AU - Cappella, Paolo
AU - Carpinelli, Patrizia
AU - Catana, Cornel
AU - Forte, Barbara
AU - Giordano, Patrizia
AU - Giorgini, Maria Laura
AU - Mantegani, Sergio
AU - Marsiglio, Aurelio
AU - Meroni, Maurizio
AU - Moll, Juergen
AU - Pittalà, Valeria
AU - Roletto, Fulvia
AU - Severino, Dino
AU - Soncini, Chiara
AU - Storici, Paola
AU - Tonani, Roberto
AU - Varasi, Mario
AU - Vulpetti, Anna
AU - Vianello, Paola
PY - 2005/4/21
Y1 - 2005/4/21
N2 - Potent and selective Aurora kinase inhibitors were identified from the combinatorial expansion of the 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole bi-cycle, a novel and versatile scaffold designed to target the ATP pocket of protein kinases. The most potent compound reported in this study had an IC 50 of 0.027 μM in the enzymatic assay for Aur-A inhibition and IC50s between 0.05 μM and 0.5 μM for the inhibition of proliferation of different tumor cell lines.
AB - Potent and selective Aurora kinase inhibitors were identified from the combinatorial expansion of the 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole bi-cycle, a novel and versatile scaffold designed to target the ATP pocket of protein kinases. The most potent compound reported in this study had an IC 50 of 0.027 μM in the enzymatic assay for Aur-A inhibition and IC50s between 0.05 μM and 0.5 μM for the inhibition of proliferation of different tumor cell lines.
UR - http://www.scopus.com/inward/record.url?scp=20944437351&partnerID=8YFLogxK
UR - http://www.scopus.com/inward/citedby.url?scp=20944437351&partnerID=8YFLogxK
U2 - 10.1021/jm049076m
DO - 10.1021/jm049076m
M3 - Article
C2 - 15828847
AN - SCOPUS:20944437351
VL - 48
SP - 3080
EP - 3084
JO - Journal of Medicinal Chemistry
JF - Journal of Medicinal Chemistry
SN - 0022-2623
IS - 8
ER -