8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one derivatives as potent, cell permeable, KDM4 (JMJD2) and KDM5 (JARID1) histone lysine demethylase inhibitors

We report the discovery of N-substituted 4-(pyridin-2-yl)thiazole-2-amine derivatives and their subsequent optimization, guided by structure-based design, to give 8-(1H-pyrazol-3-yl)pyrido[3,4-d]pyrimidin-4(3H)-ones, a series of potent JmjC histone N-methyl lysine demethylase (KDM) inhibitors which...

Full description

Bibliographic Details
Main Authors:	Bavetsias, V, Lanigan, R, Ruda, G, Atrash, B, McLaughlin, M, Tumber, A, Mok, N, Le Bihan, Y, Dempster, S, Boxall, K, Jeganathan, F, Hatch, S, Savitsky, P, Velupillai, S, Krojer, T, England, K, Sejberg, J, Thai, C, Donovan, A, Pal, A, Scozzafava, G, Bennett, J, Kawamura, A, Johansson, C, Szykowska, A, Gileadi, C, Burgess-Brown, N, von Delft, F, Oppermann, U, Walters, Z, Shipley, J, Raynaud, F, Westaway, S, Prinjha, R, Fedorov, O, Burke, R, Schofield, C, Westwood, I, Bountra, C, Müller, S, van Montfort, R, Brennan, P, Blagg, J
Format:	Journal article
Language:	English
Published:	American Chemical Society 2016

8-substituted pyrido[3,4-d]pyrimidin-4(3H)-one derivatives as potent, cell permeable, KDM4 (JMJD2) and KDM5 (JARID1) histone lysine demethylase inhibitors

Similar Items