1197196-66-9Relevant articles and documents
Discovery of a 2,4-diamino-7-aminoalkoxyquinazoline as a potent and selective inhibitor of histone lysine methyltransferase G9a
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
, p. 7950 - 7953 (2009)
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.
Quinazoline hydroxamic acid derivative and preparation method and application thereof
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Paragraph 0054; 0055-0056, (2021/03/13)
The invention relates to a quinazoline hydroxamic acid derivative and a preparation method and application thereof. The structural formula of the quinazoline hydroxamic acid derivative is as shown informula I: Y is substituted or unsubstituted aliphatic hydrocarbon group or aromatic hydrocarbon group, R1 is a nitrogen-containing substituent group, and R2 and R3 are each independently hydrogen oran alkyl group. Researches show that the compound shown in the formula I has good inhibitory activity on histone methyltransferase and histone deacetylase, can effectively inhibit tumor cell proliferation, and can be used as a lead compound for research and development of antitumor drugs.
HISTONE DEACETYLASE AND HISTONE METHYLTRANSFERASE INHIBITORS AND METHODS OF MAKING AND USE OF THE SAME
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Page/Page column 44; 49, (2018/02/28)
The compounds of formula (I) are dual inhibitors of the enzymes histone deacetylases (HDACs) and histone methyltransferase G9a, both of which are key posttranslational enzymes in cancer development.