Document Report Card

ID: ALA1137791

Journal: J Med Chem

Title: Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships.

Authors: Ermoli A, Bargiotti A, Brasca MG, Ciavolella A, Colombo N, Fachin G, Isacchi A, Menichincheri M, Molinari A, Montagnoli A, Pillan A, Rainoldi S, Sirtori FR, Sola F, Thieffine S, Tibolla M, Valsasina B, Volpi D, Santocanale C, Vanotti E.

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.

CiteXplore: 19555113

DOI: 10.1021/jm900248g