8-Substituted Pyrido[3,4-d]pyrimidin-4(3H)-one Derivatives As Potent, Cell Permeable, KDM4 (JMJD2) and KDM5 (JARID1) Histone Lysine Demethylase Inhibitors

[Image: see text] 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)...

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Detalles Bibliográficos
Autores principales: Bavetsias, Vassilios, Lanigan, Rachel M., Ruda, Gian Filippo, Atrash, Butrus, McLaughlin, Mark G., Tumber, Anthony, Mok, N. Yi, Le Bihan, Yann-Vaï, Dempster, Sally, Boxall, Katherine J., Jeganathan, Fiona, Hatch, Stephanie B., Savitsky, Pavel, Velupillai, Srikannathasan, Krojer, Tobias, England, Katherine S., Sejberg, Jimmy, Thai, Ching, Donovan, Adam, Pal, Akos, Scozzafava, Giuseppe, Bennett, James M., Kawamura, Akane, Johansson, Catrine, Szykowska, Aleksandra, Gileadi, Carina, Burgess-Brown, Nicola A., von Delft, Frank, Oppermann, Udo, Walters, Zoe, Shipley, Janet, Raynaud, Florence I., Westaway, Susan M., Prinjha, Rab K., Fedorov, Oleg, Burke, Rosemary, Schofield, Christopher J., Westwood, Isaac M., Bountra, Chas, Müller, Susanne, van Montfort, Rob L. M., Brennan, Paul E., Blagg, Julian
Formato: Online Artículo Texto
Lenguaje:English
Publicado: American Chemical Society 2016
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4770324/
https://www.ncbi.nlm.nih.gov/pubmed/26741168
http://dx.doi.org/10.1021/acs.jmedchem.5b01635

Internet

https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4770324/
https://www.ncbi.nlm.nih.gov/pubmed/26741168
http://dx.doi.org/10.1021/acs.jmedchem.5b01635

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