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J Med Chem. 2009 Dec 24;52(24):7950-3. doi: 10.1021/jm901543m.

Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a.

Author information

1
Eshelman School of Pharmacy, University of North Carolina, Chapel Hill, NC 27599, USA.

Abstract

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 cocrystal structure of G9a with a small molecule inhibitor, was obtained. The cocrystal structure validated our binding hypothesis and will enable structure-based design of novel inhibitors. 8 is a useful tool for investigating the biology of G9a and its roles in chromatin remodeling.

PMID:
19891491
PMCID:
PMC2825141
DOI:
10.1021/jm901543m
[Indexed for MEDLINE]
Free PMC Article

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