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...

Πλήρης περιγραφή

Αποθηκεύτηκε σε:
Λεπτομέρειες βιβλιογραφικής εγγραφής
Κύριοι συγγραφείς: 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
Μορφή: Artigo
Γλώσσα:Inglês
Έκδοση: 2009
Θέματα:
Article
Διαθέσιμο 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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