Discovery of an in vivo chemical probe of the lysine methyltransferases G9a and GLP

Journal of Medicinal Chemistry

Volumn 56, Issue 21, 2013, Pages 8931-8942

  Liu, Feng ^a   Barsyte Lovejoy, Dalia ^d   Li, Fengling ^d   Xiong, Yan ^a   Korboukh, Victoria ^a   Huang, Xi Ping ^b   Allali Hassani, Abdellah ^d   Janzen, William P ^a   Roth, Bryan L ^b   Frye, Stephen V ^a   Arrowsmith, Cheryl H ^d   Brown, Peter J ^d   Vedadi, Masoud ^d   Jin, Jian ^a,b,c  

^a University of North Carolina   (United States)

^b UNIVERSITY OF NORTH CAROLINA   (United States)

^c UNIVERSITY OF NORTH CAROLINA SCHOOL OF MEDICINE   (United States)

^d UNIVERSITY OF TORONTO   (Canada)

Author keywords

[No Author keywords available]

Indexed keywords

2 (4,4 DIFLUOROPIPERIDIN 1 YL) N (1 ISOPROPYLPIPERIDIN 4 YL) 6 METHOXY 7 (3 (PYRROLIDIN 1 YL)PROPOXY)QUINAZOLIN 4 AMINE; 2 CYCLOHEXYL N (1 ISOPROPYL 4 PIPERIDINYL) 6 METHOXY 7 [3 (1 PYRROLIDINYL)PROPOXY] 4 QUINAZOLINAMINE; 4 (4 ((1 CYCLOPROPYLPIPERIDIN 4 YL)AMINO) 6 METHOXY 7 (3 (PYRROLIDIN 1 YL)PROPOXY)QUINAZOLIN 2 YL)THIOMORPHOLINE 1,1 DIOXIDE; 4 (4 ((1 ISOPROPYLPIPERIDIN 4 YL)AMINO) 6 METHOXY 7 (3 (PYRROLIDIN 1 YL)PROPOXY)QUINAZOLIN 2 YL)THIOMORPHOLINE 1,1 DIOXIDE; 4 CHLORO 2 CYCLOHEXYL 7 (3 (4,4 DIFLUOROPIPERIDIN 1 YL) PROPOXY) 6 METHOXYQUINAZOLINE; 4 CHLORO 6 METHOXY 2 (PHOSPHINAN 4 YL) 7 (3 (PYRROLIDIN 1 YL)PROPOXY)QUINAZOLINE; 4 CHLORO 7 (3 (4,4 DIFLUOROPIPERIDIN 1 YL)PROPOXY) 6 METHOXY 2 (PIPERIDIN 1 YL)QUINAZOLINE; 7 (3 (4,4 DIFLUOROPIPERIDIN 1 YL)PROPOXY) N (1 ISOPROPYLPIPERIDIN 4 YL) 6 METHOXY 2 (TETRAHYDRO 2H PYRAN 4 YL) QUINAZOLIN 4 AMINE; 7 (3 (4,4 DIFLUOROPIPERIDIN 1YL)PROPOXY) N (1 ISOPROPYLPIPERIDIN 4 YL) 6 METHOXY 2 CYCLOHEXYLQUINAZOLIN 4 AMINE; CYTOCHROME P450; HISTONE H3; HISTONE LYSINE METHYLTRANSFERASE; HISTONE LYSINE METHYLTRANSFERASE INHIBITOR; LYSINE METHYLTRANSFERASE G9A; LYSINE METHYLTRANSFERASE GLP; METHYL 2 AMINO 4 (3 (4,4 DIFLUOROPIPERIDIN 1 YL)PROPOXY) 5 METHOXYBENZOATE; N (1 CYCLOPROPYLPIPERIDIN 4 YL) 2 (4,4 DIFLUOROPIPERIDIN 1 YL) 6 METHOXY 7 (3 (PYRROLIDIN 1 YL)PROPOXY)QUINAZOLIN 4 AMINE; N (1 ISOPROPYLPIPERIDIN 4 YL) 6 METHOXY 2 MORPHOLINO 7 (3 (PYRROLIDIN 1 YL)PROPOXY)QUINAZOLIN 4 AMINE; N (1 ISOPROPYLPIPERIDIN 4 YL) 6 METHOXY 7 (3 (PYRROLIDIN 1 YL)PROPOXY) 2 (3,3,4,4 TETRAFLUOROPYRROLIDIN 1 YL)QUINAZOLIN 4 AMINE; N (1 ISOPROPYLPIPERIDIN 4 YL) 6 METHOXY 7 (3 (PYRROLIDIN 1 YL)PROPOXY) 2 (TETRAHYDRO 2H PYRAN 4 YL)QUINAZOLIN 4 AMINE; UNC 0642; UNCLASSIFIED DRUG;

ANIMAL EXPERIMENT; ARTICLE; CYTOTOXICITY; DRUG STRUCTURE; DRUG SYNTHESIS; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HISTONE METHYLATION; IC 50; IN VIVO STUDY; MALE; MICHAELIS MENTEN KINETICS; MOUSE; NONHUMAN; STRUCTURE ACTIVITY RELATION;

ANIMALS; ANTINEOPLASTIC AGENTS; CELL LINE, TUMOR; CELL PROLIFERATION; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DISCOVERY; DRUG SCREENING ASSAYS, ANTITUMOR; ENZYME INHIBITORS; HISTOCOMPATIBILITY ANTIGENS; HISTONE-LYSINE N-METHYLTRANSFERASE; HUMANS; MALE; MICE; MOLECULAR STRUCTURE; STRUCTURE-ACTIVITY RELATIONSHIP;

EID: 84887923349     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/jm401480r     Document Type: Article

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