The present invention relates to compounds that inhibit activity of the histone lysine N-methyltransferase, Enhancer of Zeste Homolog 2 (EZH2), pharmaceutical compositions comprising the compounds, and methods of using the compounds to treat cancer, such as hematologic and solid tumors.本發明係關於抑制組蛋白離胺酸N-甲基轉移酶(Zeste同源物增強子2;EZH2)活性之化合物、包含該等化合物之醫藥組合物及使用該等化合物治療諸如血液及實體腫瘤之癌症的方法。