Discovery of a 2,4-Diamino-7-aminoalkoxy-quinazoline as a Potent and Selective Inhibitor of Histone Lysine Methyltransferase G9a

SAR exploration of the 2,4-diamino-6,7-dimethoxyquinazoline template led to the discovery of 8 (UNC0224) as a potent and selective G9a inhibitor. A high resolution X-ray crystal structure of the G9a-8 complex, the first co-crystal structure of G9a with a small molecule inhibitor, was obtained. The c...

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Main Authors: Liu, Feng, Chen, Xin, Allali-Hassani, Abdellah, Quinn, Amy M., Wasney, Gregory A., Dong, Aiping, Barsyte, Dalia, Kozieradzki, Ivona, Senisterra, Guillermo, Chau, Irene, Siarheyeva, Alena, Kireev, Dmitri B., Jadhav, Ajit, Herold, J. Martin, Frye, Stephen V., Arrowsmith, Cheryl H., Brown, Peter J., Simeonov, Anton, Vedadi, Masoud, Jin, Jian
Formato: Artigo
Idioma:Inglês
Publicado em: 2009
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Article
Acesso em linha:https://ncbi.nlm.nih.gov/pmc/articles/PMC2825141/
https://ncbi.nlm.nih.gov/pubmed/19891491
https://ncbi.nlm.nih.govhttp://dx.doi.org/10.1021/jm901543m
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