1. Cell division cycle 7 kinase inhibitors: 1H-pyrrolo[2,3-b]pyridines, synthesis and structure-activity relationships
- Author
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Ermoli, A, Bargiotti, A, Brasca, M, Ciavolella, A, Colombo, N, Fachin, G, Isacchi, A, Menichincheri, M, Molinari, A, Montagnoli, A, Pillan, A, Rainoldi, S, Sirtori, F, Sola, F, Thieffine, S, Tibolla, M, Valsasina, B, Volpi, D, Santocanale, C, Vanotti, E, Brasca, MG, COLOMBO, NICOLETTA, Sirtori, FR, Vanotti, E., Ermoli, A, Bargiotti, A, Brasca, M, Ciavolella, A, Colombo, N, Fachin, G, Isacchi, A, Menichincheri, M, Molinari, A, Montagnoli, A, Pillan, A, Rainoldi, S, Sirtori, F, Sola, F, Thieffine, S, Tibolla, M, Valsasina, B, Volpi, D, Santocanale, C, Vanotti, E, Brasca, MG, COLOMBO, NICOLETTA, Sirtori, FR, and 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
- Published
- 2009