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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Autori principali: 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
Natura: Artigo
Lingua:Inglês
Pubblicazione: 2009
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Article
Accesso online: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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