The present invention relates to compounds that inhibit activity of the histone lysine 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甲基轉移酶(Zeste增強子同源物2;EZH2)之活性之化合物、包含該等化合物之醫藥組合物,及使用該等化合物治療癌症(諸如血液學及實體腫瘤)之方法。