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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主要な著者: 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
フォーマット: Artigo
言語:Inglês
出版事項: 2009
主題:
Article
オンライン･アクセス: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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