| Literature DB >> 19555113 |
Antonella Ermoli1, Alberto Bargiotti, Maria Gabriella Brasca, Antonella Ciavolella, Nicoletta Colombo, Gabriele Fachin, Antonella Isacchi, Maria Menichincheri, Antonio Molinari, Alessia Montagnoli, Antonio Pillan, Sonia Rainoldi, Federico Riccardi Sirtori, Francesco Sola, Sandrine Thieffine, Marcellino Tibolla, Barbara Valsasina, Daniele Volpi, Corrado Santocanale, Ermes Vanotti.
Abstract
Cdc7 kinase has recently emerged as an attractive target for cancer therapy and low-molecular-weight inhibitors of Cdc7 kinase have been found to be effective in the inhibition of tumor growth in animal models. In this paper, we describe synthesis and structure-activity relationships of new 1H-pyrrolo[2,3-b]pyridine derivatives identified as inhibitors of Cdc7 kinase. Progress from (Z)-2-phenyl-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-3,5-dihydro-4H-imidazol-4-one (1) to [(Z)-2-(benzylamino)-5-(1H-pyrrolo[2,3-b]pyridin-3-ylmethylene)-1,3-thiazol-4(5H)-one] (42), a potent ATP mimetic inhibitor of Cdc7 kinase with IC(50) value of 7 nM, is also reported.Entities:
Mesh:
Substances:
Year: 2009 PMID: 19555113 DOI: 10.1021/jm900248g
Source DB: PubMed Journal: J Med Chem ISSN: 0022-2623 Impact factor: 7.446