1346575-64-1Relevant academic research and scientific papers
EZH2 inhibitor as well as preparation of EZH2 inhibitor and application of EZH2 inhibitor in anti-tumor treatment
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, (2019/08/20)
The invention discloses an EZH2 inhibitor as well as preparation of the EZH2 inhibitor and application of the EZH2 inhibitor in anti-tumor treatment. The EZH2 inhibitor has a structure represented bya general formula I shown in the description, wherein de
SULFONYL-SUBSTITUTED BENZOHETEROCYCLIC DERIVATIVE, PREPARATION METHOD AND MEDICAL USE THEREOF
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Paragraph 0138; 0158, (2019/10/23)
The present invention relates to a sulfonyl-substituted benzoheterocyclic derivative, a preparation method and medical use thereof. Particularly, disclosed is a compound of formula (I) or a pharmaceutically acceptable salt, stereoisomer, solvate, or prodrug thereof, and a preparation method and application thereof. The definition of each group in the formula can be found in the specification and the claims.
EZH2 INHIBITORS AND USES THEREOF
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, (2016/07/05)
The present disclosure provides compounds of any one of Formulae (I) and (II). The compounds described herein are inhibitors of histone methyltransferases (e.g., enhancer of zeste homolog 1 (EZH1) and enhancer of zeste homolog 2 (EZH2)) and are useful in treating and/or preventing a broad range of diseases (e.g., proliferative diseases). Also provided in the present disclosure are pharmaceutical compositions, kits, methods, and uses including or using a compound described herein. Further provided in the present disclosure are methods of identifying EZH1and/or EZH2 inhibitors.
METHOD OF TREATMENT
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Paragraph 0730; 0735, (2014/09/29)
The present invention relates to a method of treating T cell mediated inflammatory immune diseases or T cell mediated hypersensitivity diseases, which comprises administering to a human in need thereof an effective amount of a compound which inhibits EZH2 and/or EZH1, or a pharmaceutically acceptable salt thereof.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00155; 00156, (2014/10/04)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
ENHANCER OF ZESTE HOMOLOG 2 INHIBITORS
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Page/Page column 45; 46; 47, (2013/12/03)
This invention relates to novel substituted benzamide according to Formula (I) which are inhibitors of Enhancer of Zeste Homolog 2 (EZH2), to pharmaceutical compositions containing them, to processes for their preparation, and to their use in therapy for the treatment of cancers.
Identification of potent, selective, cell-Active inhibitors of the histone lysine methyltransferase EZH2
Verma, Sharad K.,Tian, Xinrong,Lafrance, Louis V.,Duquenne, Céline,Suarez, Dominic P.,Newlander, Kenneth A.,Romeril, Stuart P.,Burgess, Joelle L.,Grant, Seth W.,Brackley, James A.,Graves, Alan P.,Scherzer, Daryl A.,Shu, Art,Thompson, Christine,Ott, Heidi M.,Van Aller, Glenn S.,MacHutta, Carl A.,Diaz, Elsie,Jiang, Yong,Johnson, Neil W.,Knight, Steven D.,Kruger, Ryan G.,McCabe, Michael T.,Dhanak, Dashyant,Tummino, Peter J.,Creasy, Caretha L.,Miller, William H.
supporting information, p. 1091 - 1096 (2013/02/23)
The histone H3-lysine 27 (H3K27) methyltransferase EZH2 plays a critical role in regulating gene expression, and its aberrant activity is linked to the onset and progression of cancer. As part of a drug discovery program targeting EZH2, we have identified highly potent, selective, SAM-competitive, and cell-Active EZH2 inhibitors, including GSK926 (3) and GSK343 (6). These compounds are small molecule chemical tools that would be useful to further explore the biology of EZH2.
