First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.

@article{Menichincheri2009FirstCK,
  title={First Cdc7 kinase inhibitors: pyrrolopyridinones as potent and orally active antitumor agents. 2. Lead discovery.},
  author={Maria Menichincheri and Alberto Bargiotti and J. E. Berthelsen and Jay Aaron Bertrand and Roberto Tiberio Bossi and Antonella Ciavolella and Alessandra Cirla and Cinzia Cristiani and Valter Croci and Roberto D'Alessio and Marina Fasolini and Francesco Fiorentini and B. de C. Forte and Antonella Isacchi and Katia Martina and Antonio Molinari and Alessia Montagnoli and Paolo Orsini and Fabrizio Orzi and Enrico Pesenti and Daniele Pezzetta and Antonio Pillan and Italo Poggesi and Fulvia Roletto and Alessandra Scolaro and Marco Tat{\`o} and Marcellino Tibolla and Barbara Valsasina and Mario Varasi and Daniele Volpi and Corrado Santocanale and Ermes Vanotti},
  journal={Journal of medicinal chemistry},
  year={2009},
  volume={52 2},
  pages={293-307}
}
Cdc7 kinase is a key regulator of the S-phase of the cell cycle, known to promote the activation of DNA replication origins in eukaryotic organisms. Cdc7 inhibition can cause tumor-cell death in a p53-independent manner, supporting the rationale for developing Cdc7 inhibitors for the treatment of cancer. In this paper, we conclude the structure-activity relationships study of the 2-heteroaryl-pyrrolopyridinone class of compounds that display potent inhibitory activity against Cdc7 kinase… CONTINUE READING