From adenosine and 2′-C-Me adenosine, a 3-step route towards nucleoside DOT1L inhibitors, including pinometostat, EPZ5677, and FED1, was established. With useful structural-activity relationship information, the newly prepared 2′-C-Me adenosine derivatives contribute to the limited repertoire of ribose-modified nucleoside DOT1L inhibitors. In general, this new synthetic method will facilitate not only the study of nucleoside DOT1L inhibitors, but also the synthetic and medicinal chemistry research of 5′-deoxy-5′-amino adenosine derivatives.

中文翻译：

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抑癌药及相关5'-脱氧-5'-氨基腺苷衍生物的简便制备及其对DOT1L的活性

从腺苷和2'- C- Me腺苷，建立了向核苷DOT1L抑制剂（包括匹诺司他，EPZ5677和FED1）的3步路线。借助有用的结构活性关系信息，新制备的2'- C- Me腺苷衍生物有助于限制核糖修饰的核苷DOT1L抑制剂的库。通常，这种新的合成方法不仅将有助于核苷DOT1L抑制剂的研究，而且将促进5'-脱氧-5'-氨基腺苷衍生物的合成和药物化学研究。