Synthesis and Structure–Activity Relationship Investigation of Adenosine-Containing Inhibitors of Histone Methyltransferase DOT1L

Histone3-lysine79 (H3K79) methyltransferase DOT1L has been found to be a drug target for acute leukemia with MLL (mixed lineage leukemia) gene translocations. A total of 55 adenosine-containing compounds were designed and synthesized, among which several potent DOT1L inhibitors were identified with...

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Veröffentlicht in:	Journal of medicinal chemistry 2012-09, Vol.55 (18), p.8066-8074
Hauptverfasser:	Anglin, Justin L, Deng, Lisheng, Yao, Yuan, Cai, Guobin, Liu, Zhen, Jiang, Hong, Cheng, Gang, Chen, Pinhong, Dong, Shuo, Song, Yongcheng
Format:	Artikel
Sprache:	eng
Schlagworte:	Adenosine - chemical synthesis Adenosine - chemistry Adenosine - metabolism Adenosine - pharmacology Chemistry Techniques, Synthetic Drug Design Enzyme Inhibitors - chemical synthesis Enzyme Inhibitors - chemistry Enzyme Inhibitors - metabolism Enzyme Inhibitors - pharmacology Humans Methyltransferases - antagonists & inhibitors Methyltransferases - chemistry Methyltransferases - metabolism Molecular Docking Simulation Protein Conformation Structure-Activity Relationship
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