Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L.

@article{Anglin2012SynthesisAS,
  title={Synthesis and structure-activity relationship investigation of adenosine-containing inhibitors of histone methyltransferase DOT1L.},
  author={Justin L. Anglin and Lisheng Deng and Yuan Yao and Guobin Cai and Zhen Liu and Hong Jiang and Gang Cheng and Pinhong Chen and Shuo Dong and Yongcheng Song},
  journal={Journal of medicinal chemistry},
  year={2012},
  volume={55 18},
  pages={
          8066-74
        }
}
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 K(i) values as low as 0.5 nM. These compounds also show high selectivity (>4500-fold) over three other histone methyltransferases. Structure-activity relationships (SAR) of these compounds for their… CONTINUE READING
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