Protein lysine methyltransferase G9a inhibitors: design, synthesis, and structure activity relationships of 2, 4-diamino-7-aminoalkoxy-quinazolines.

F Liu, X Chen, A Allali-Hassani, AM Quinn…

文献索引：Liu, Feng; Chen, Xin; Allali-Hassani, Abdellah; Quinn, Amy M.; Wigle, Tim J.; Wasney, Gregory A.; Dong, Aiping; Senisterra, Guillermo; Chau, Irene; Siarheyeva, Alena; Norris, Jacqueline L.; Kireev, Dmitri B.; Jadhav, Ajit; Herold, J. Martin; Janzen, William P.; Arrowsmith, Cheryl H.; Frye, Stephen V.; Brown, Peter J.; Simeonov, Anton; Vedadi, Masoud; Jin, Jian Journal of Medicinal Chemistry, 2010 , vol. 53, # 15 p. 5844 - 5857

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被引用次数: 111

摘要

Protein lysine methyltransferase G9a, which catalyzes methylation of lysine 9 of histone H3 (H3K9) and lysine 373 (K373) of p53, is overexpressed in human cancers. Genetic knockdown of G9a inhibits cancer cell growth, and the dimethylation of p53 K373 results in the inactivation of p53. Initial SAR exploration of the 2, 4-diamino-6, 7-dimethoxyquinazoline template represented by 3a (BIX01294), a selective small molecule inhibitor of G9a and ...