title: Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.
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.
authors: Nerviano Medical Sciences, 20014 Nerviano, Milano, Italy.
authors: Antonella
authors: A
authors: Ermoli
authors: Alberto
authors: A
authors: Bargiotti
authors: Maria Gabriella
authors: MG
authors: Brasca
authors: Antonella
authors: A
authors: Ciavolella
authors: Nicoletta
authors: N
authors: Colombo
authors: Gabriele
authors: G
authors: Fachin
authors: Antonella
authors: A
authors: Isacchi
authors: Maria
authors: M
authors: Menichincheri
authors: Antonio
authors: A
authors: Molinari
authors: Alessia
authors: A
authors: Montagnoli
authors: Antonio
authors: A
authors: Pillan
authors: Sonia
authors: S
authors: Rainoldi
authors: Federico Riccardi
authors: FR
authors: Sirtori
authors: Francesco
authors: F
authors: Sola
authors: Sandrine
authors: S
authors: Thieffine
authors: Marcellino
authors: M
authors: Tibolla
authors: Barbara
authors: B
authors: Valsasina
authors: Daniele
authors: D
authors: Volpi
authors: Corrado
authors: C
authors: Santocanale
authors: Ermes
authors: E
authors: Vanotti
mesh_terms: D018797:Cell Cycle Proteins / Q000037:antagonists & inhibitors* / Q000737:chemistry; D002460:Cell Line; D006801:Humans; D008958:Models, Molecular; D008968:Molecular Conformation; D047428:Protein Kinase Inhibitors / Q000031:analogs & derivatives / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D017346:Protein Serine-Threonine Kinases / Q000037:antagonists & inhibitors* / Q000737:chemistry; D011725:Pyridines / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D013329:Structure-Activity Relationship
chemical_list: D018797:Cell Cycle Proteins; D047428:Protein Kinase Inhibitors; D011725:Pyridines; C068619:CDC7 protein, human; D017346:Protein Serine-Threonine Kinases