1802175-06-9Relevant articles and documents
SUBSTITUTED BENZENE AND 6,5-FUSED BICYCLIC HETEROARYL COMPOUNDS
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, (2016/05/02)
The present invention relates to substituted benzene compounds and bicyclic heteroaryl compounds. The present invention also relates to pharmaceutical compositions containing these compounds and methods of treating cancer by administering these compounds and pharmaceutical compositions to subjects in need thereof. The present invention also relates to the use of such compounds for research or other non-therapeutic purposes.
Discovery, design, and synthesis of indole-based EZH2 inhibitors
Gehling, Victor S.,Vaswani, Rishi G.,Nasveschuk, Christopher G.,Duplessis, Martin,Iyer, Priyadarshini,Balasubramanian, Srividya,Zhao, Feng,Good, Andrew C.,Campbell, Robert,Lee, Christina,Dakin, Les A.,Cook, Andrew S.,Gagnon, Alexandre,Harmange, Jean-Christophe,Audia, James E.,Cummings, Richard T.,Normant, Emmanuel,Trojer, Patrick,Albrecht, Brian K.
, p. 3644 - 3649 (2015/08/11)
The discovery and optimization of a series of small molecule EZH2 inhibitors is described. Starting from dimethylpyridone HTS hit (2), a series of indole-based EZH2 inhibitors were identified. Biochemical potency and microsomal stability were optimized during these studies and afforded compound 22. This compound demonstrates nanomolar levels of biochemical potency (IC50 = 0.002 μM), cellular potency (EC50 = 0.080 μM), and afforded tumor regression when dosed (200 mpk SC BID) in an EZH2 dependent tumor xenograft model.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 0082; 0083, (2014/08/20)
Agents having the structural Formula (II) for modulating histone methyl modifying enzymes, compositions and uses thereof for instance as anti-cancer agents are provided herein.
MODULATORS OF METHYL MODIFYING ENZYMES, COMPOSITIONS AND USES THEREOF
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Paragraph 00308; 00309, (2013/08/28)
Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.