The present invention provides novel compounds of Formula (I), and pharmaceutically compositions thereof. Compounds of Formula (I) are inhibitors of histone deacetylases (HDACs) and 3-hydroxy-3-methylglutaryl coenzyme A (HMG-CoA) reductase (HMGR). Also provided are methods of using the compounds and pharmaceutical compositions for inhibiting the activity of HDACs and HMGR, treating diseases associated with HDACs or HMGR (e.g., cancer, hypercholesterolemia, an acute or chronic inflammatory disease, autoimmune disease, allergic disease, pathogen infection, neurodegenerative disease, and a disease associated with oxidative stress), or inhibiting drug resistance of cancer cells.本發明提供一種新穎的式(I)化合物及包含此新穎式(I)化合物的藥學組合物。此式(I)化合物是組蛋白去乙醯酶(HDACs)和3-羥基-3-甲基戊二醯基輔酶A(HMG-CoA)還原酶(HMGR)的抑制劑。同時,本發明還提供以此式(I)化合物及藥學組合物來抑制HDACs和HMGR活性、治療與HDACs和HMGR相關疾病(如,癌症、高膽固醇血症、急性或慢性發炎、自體免疫疾病、過敏性疾病、病源菌感染、神經退化疾病、與氧化壓力相關的疾病)或是抑制癌細胞抗藥性的方法,