Discovery of First-in-Class, Potent, and Orally Bioavailable Embryonic Ectoderm Development (EED) Inhibitor with Robust Anticancer Efficacy

Journal of Medicinal Chemistry

Volumn 60, Issue 6, 2017, Pages 2215-2226

  Huang, Ying ^a   Zhang, Jeff ^a   Yu, Zhengtian ^a   Zhang, Hailong ^a,e   Wang, Youzhen ^a,c   Lingel, Andreas ^b,c   Qi, Wei ^a   Gu, Justin ^a   Zhao, Kehao ^a,c   Shultz, Michael D ^a,c   Wang, Long ^a   Fu, Xingnian ^a   Sun, Yongfeng ^a   Zhang, Qiong ^a   Jiang, Xiangqing ^a   Zhang, Jiangwei ^a   Zhang, Chunye ^a   Li, Ling ^a   Zeng, Jue ^a   Feng, Lijian ^a   Zhang, Chao ^a,f   Liu, Yueqin ^a,f   Zhang, Man ^a   Zhang, Lijun ^a   Zhao, Mengxi ^a   Gao, Zhenting ^a   Liu, Xianghui ^a,g   Fang, Douglas ^a   Guo, Haibing ^a,f   Mi, Yuan ^a   Gabriel, Tobias ^a,c   Dillon, Michael P ^b,d   Atadja, Peter ^a   Oyang, Counde ^a   more..

^a Novartis Institutes for BioMedical Research ^*

^b Novartis Institutes for Biomedical Research   (China)

^c NOVARTIS INSTITUTES FOR BIOMEDICAL RESEARCH   (United States)

^d IDEAYA Biosciences Inc   (United States)

^e Array Bio Pharma Inc   (United States)

^f Roche R and D (China) Center   (China)

^g National University of Singapore   (Singapore)

Author keywords

[No Author keywords available]

Indexed keywords

ANTINEOPLASTIC AGENT; EMBRYONIC ECTODERM DEVELOPMENT PROTEIN; N (FURAN 2 YLMETHYL) 8 [4 (METHYLSULFONYL)PHENYL][1,2,4]TRIAZOLO[4,3 C]PYRIMIDIN 5 AMINE; POLYCOMB REPRESSIVE COMPLEX 2; TRANSCRIPTION FACTOR EZH2; UNCLASSIFIED DRUG; EED PROTEIN, HUMAN; EED226; HISTONE; LYSINE; SULFONE; TRIAZOLE DERIVATIVE;

ANIMAL CELL; ANIMAL EXPERIMENT; ANIMAL MODEL; ANIMAL TISSUE; ANTINEOPLASTIC ACTIVITY; ANTIPROLIFERATIVE ACTIVITY; AREA UNDER THE CURVE; ARTICLE; CACO-2 CELL LINE; CANCER MODEL; CONFORMATIONAL TRANSITION; CONTROLLED STUDY; CRYSTAL STRUCTURE; DIFFUSE LARGE B CELL LYMPHOMA; DRUG BIOAVAILABILITY; DRUG CLEARANCE; DRUG EFFICACY; ENZYME ACTIVE SITE; FEMALE; HEPATIC CLEARANCE; IC50; LIVER MICROSOME; MALE; MOUSE; NONHUMAN; PLASMA PROTEIN BINDING; TUMOR REGRESSION; TUMOR XENOGRAFT; X RAY CRYSTALLOGRAPHY; ANIMAL; ANTAGONISTS AND INHIBITORS; BAGG ALBINO MOUSE; CELL PROLIFERATION; CHEMISTRY; DOG; DRUG EFFECTS; HAPLORHINI; HUMAN; LYMPHOMA, LARGE B-CELL, DIFFUSE; METABOLISM; METHYLATION; MOLECULAR DOCKING; NUDE MOUSE; RAT;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL PROLIFERATION; CRYSTALLOGRAPHY, X-RAY; DOGS; FEMALE; HAPLORHINI; HISTONES; HUMANS; LYMPHOMA, LARGE B-CELL, DIFFUSE; LYSINE; MALE; METHYLATION; MICE; MICE, INBRED BALB C; MICE, NUDE; MOLECULAR DOCKING SIMULATION; POLYCOMB REPRESSIVE COMPLEX 2; RATS; SULFONES; TRIAZOLES;

EID: 85016316160     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.6b01576     Document Type: Article

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