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Histone methyltransferase DOT1L is a drug target for MLL leukemia. We report an efficient synthesis of a cyclopentane-containing compound that potently and selectively inhibits DOT1L (K i = 1.1 nM) as well as H3K79 methylation (IC 50 ~ 200 nM). Importantly, this compound exhibits a high stability in plasma and liver microsomes, suggesting it is a better drug candidate.

Synthesis, activity and metabolic stability of non-ribose containing inhibitors of histone methyltransferase DOT1L