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...

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मुख्य लेखकों:	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
स्वरूप:	Journal article
भाषा:	English
प्रकाशित:	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

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