Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.

  title={Optimization of cellular activity of G9a inhibitors 7-aminoalkoxy-quinazolines.},
  author={F. Liu and D. Barsyte-Lovejoy and Abdellah Allali-Hassani and Yunlong He and J. Herold and X. Chen and C. M. Yates and S. Frye and P. Brown and Jing Huang and M. Vedadi and C. Arrowsmith and J. Jin},
  journal={Journal of medicinal chemistry},
  volume={54 17},
  • F. Liu, D. Barsyte-Lovejoy, +10 authors J. Jin
  • Published 2011
  • Chemistry, Medicine
  • Journal of medicinal chemistry
  • Protein lysine methyltransferase G9a plays key roles in the transcriptional repression of a variety of genes via dimethylation of lysine 9 on histone H3 (H3K9me2) of chromatin as well as dimethylation of nonhistone proteins including tumor suppressor p53. We previously reported the discovery of UNC0321 (3), the most potent G9a inhibitor to date, via structure-based design and structure-activity relationship (SAR) exploration of the quinazoline scaffold represented by BIX01294 (1). Despite its… CONTINUE READING
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