1009056-19-2Relevant articles and documents
Cdc7 kinase inhibitors: Pyrrolopyridinones as potential antitumor agents. 1. Synthesis and structure-activity relationships
Vanotti, Ermes,Amici, Raffaella,Bargiotti, Alberto,Berthelsen, Jens,Bosotti, Roberta,Ciavolella, Antonella,Cirla, Alessandra,Cristiani, Cinzia,D'Alessio, Roberto,Forte, Barbara,Isacchi, Antonella,Martina, Katia,Menichincheri, Maria,Molinari, Antonio,Montagnoli, Alessia,Orsini, Paolo,Pillan, Antonio,Roletto, Fulvia,Scolaro, Alessandra,Tibolla, Marcellino,Valsasina, Barbara,Varasi, Mario,Volpi, Daniele,Santocanale, Corrado
, p. 487 - 501 (2008/09/18)
Cdc7 kinase is an essential protein that promotes DNA replication in eukaryotic organisms. Genetic evidence indicates that Cdc7 inhibition can cause selective tumor-cell death in a p53-independent manner, supporting the rationale for developing Cdc7 small-molecule inhibitors for the treatment of cancers. In this paper, the synthesis and structure-activity relationships of 2-heteroaryl-pyrrolopyridinones, the first potent Cdc7 kinase inhibitors, are described. Starting from 2-pyridin-4-yl-1,5,6,7-tetrahydro-pyrrolo[3,2-c] pyridin-4-one, progress toward a simple scaffold, tailored for Cdc7 inhibition, is reported.