Design, synthesis, and structure-activity relationship of novel lsd1 inhibitors based on pyrimidine-thiourea hybrids as potent, orally active antitumor agents

Journal of Medicinal Chemistry

Volumn 58, Issue 4, 2015, Pages 1705-1716

  Ma, Li Ying ^a   Zheng, Yi Chao ^a   Wang, Sai Qi ^a   Wang, Bo ^a   Wang, Zhi Ru ^a   Pang, Lu Ping ^a   Zhang, Miao ^a   Wang, Jun Wei ^a   Ding, Lina ^a   Li, Juan ^a   Wang, Cong ^a   Hu, Biao ^a   Liu, Ying ^a   Zhang, Xiao Dan ^a   Wang, Jia Jia ^a   Wang, Zhi Jian ^a   Zhao, Wen ^a   Liu, Hong Min ^a  

^a ZHENGZHOU UNIVERSITY   (China)

Author keywords

[No Author keywords available]

Indexed keywords

2 (5 CYANO 2 (PROP 2 YN 1 YLTHIO) 6 (4 TOLYL)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 2 (5 CYANO 2 (PROP 2 YN 1 YLTHIO) 6 (4 TOLYL)PYRIMIDIN 4 YL)HYDRAZINECARBOXAMIDE; 2 (5 CYANO 6 (3,4 DIFLUOROPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 2 (5 CYANO 6 (4 FLUOROPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 2 (5 CYANO 6 (4 ISOPROPYLPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 2 (5 CYANO 6 (4 NITROPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 2 (5 CYANO 6 (4 NITROPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4YL)HYDRAZINECARBOTHIOAMIDE; 2 (5 CYANO 6 PHENYL 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 2 (6 (3 CHLOROPHENYL) 5 CYANO 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 2 (6 (4 BROMOPHENYL) 5 CYANO 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 2 (6 (4 CHLOROPHENYL) 5 CYANO 2 (PROP 2 YN 1 YLTHIO)PYRIMIDIN 4 YL)HYDRAZINECARBOTHIOAMIDE; 4 (4 CHLOROPHENYL) 2 (PROP 2 YN 1 YLTHIO) 6 ((3 (TRIFLUOROMETHYL)PHENYL)AMINO)PYRIMIDINE 5 CARBONITRILE; 4 CHLORO 2 (PROP 2 YN 1 YLTHIO) 6 (3,4,5 TRIMETHOXYPHENYL)PYRIMIDINE 5 CARBONITRILE; 4 CHLORO 2 (PROP 2 YN 1 YLTHIO) 6 (4 TOLYL)PYRIMIDINE 5 CARBONITRILE; 4 CHLORO 6 (3,4 DIFLUOROPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDINE 5 CARBONITRILE; 4 CHLORO 6 (4 CHLOROPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDINE 5 CARBONITRILE; 4 CHLORO 6 (4 ISOPROPYLPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDINE 5 CARBONITRILE; 4 CHLORO 6 (4 NITROPHENYL) 2 (PROP 2 YN 1 YLTHIO)PYRIMIDINE 5 CARBONITRILE; 4 CHLORO 6 PHENYL 2 (PROP 2 YN 1 YLTHIO)PYRIMIDINE 5 CARBONITRILE; ANTINEOPLASTIC AGENT; HISTONE LYSINE SPECIFIC DEMETHYLASE 1 INHIBITOR; OXYGENASE INHIBITOR; PYRIMIDINE DERIVATIVE; THIOUREA DERIVATIVE; UNCLASSIFIED DRUG; ENZYME INHIBITOR; HISTONE DEMETHYLASE; KDM1A PROTEIN, HUMAN; PYRIMIDINE; THIOUREA;

ANTINEOPLASTIC ACTIVITY; ARTICLE; CELL MIGRATION; CONTROLLED STUDY; DRUG DESIGN; DRUG SYNTHESIS; GASTRIC CANCER CELL LINE; HUMAN; HUMAN CELL; IN VITRO STUDY; IN VIVO STUDY; STRUCTURE ACTIVITY RELATION; ANIMAL; ANTAGONISTS AND INHIBITORS; APOPTOSIS; BAGG ALBINO MOUSE; C57BL MOUSE; CELL PROLIFERATION; CELL SURVIVAL; CHEMICAL STRUCTURE; CHEMISTRY; DOSE RESPONSE; DRUG EFFECTS; DRUG SCREENING; MALE; METABOLISM; MOUSE; NEOPLASMS, EXPERIMENTAL; ORAL DRUG ADMINISTRATION; PATHOLOGY; TUMOR CELL LINE;

ADMINISTRATION, ORAL; ANIMALS; ANTINEOPLASTIC AGENTS; APOPTOSIS; CELL LINE, TUMOR; CELL PROLIFERATION; CELL SURVIVAL; DOSE-RESPONSE RELATIONSHIP, DRUG; DRUG DESIGN; DRUG SCREENING ASSAYS, ANTITUMOR; ENZYME INHIBITORS; HISTONE DEMETHYLASES; HUMANS; MALE; MICE; MICE, INBRED BALB C; MICE, INBRED C57BL; MOLECULAR STRUCTURE; NEOPLASMS, EXPERIMENTAL; PYRIMIDINES; STRUCTURE-ACTIVITY RELATIONSHIP; THIOUREA;

EID: 84924023636     PISSN: 00222623     EISSN: 15204804     Source Type: Journal    
DOI: 10.1021/acs.jmedchem.5b00037     Document Type: Article

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