| Literature DB >> 18201066 |
Ermes Vanotti1, Raffaella Amici, Alberto Bargiotti, Jens Berthelsen, Roberta Bosotti, Antonella Ciavolella, Alessandra Cirla, Cinzia Cristiani, Roberto D'Alessio, Barbara Forte, Antonella Isacchi, Katia Martina, Maria Menichincheri, Antonio Molinari, Alessia Montagnoli, Paolo Orsini, Antonio Pillan, Fulvia Roletto, Alessandra Scolaro, Marcellino Tibolla, Barbara Valsasina, Mario Varasi, Daniele Volpi, Corrado Santocanale.
Abstract
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.Entities:
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Year: 2008 PMID： 18201066 DOI： 10.1021/jm700956r
Source DB: PubMed Journal: J Med Chem ISSN： 0022-2623 Impact factor: 7.446