The invention relates to the field of medicinal chemistry, and in particular, relates to an application of a brefeldin A ester derivative in inhibiting tumor proliferation activity, wherein the structure of the brefeldin A ester derivative is represented by a formula (I). The novel compound has outstanding effects in preventing or treating hyperproliferative diseases including liver cancer, leukemia, breast cancer, colonic adenocarcinoma, gastric cancer, lung cancer, Bartter's esophagus cancer, cervical cancer, pancreatic cancer, endometrial cancer, bone cancer, lymph cancer, kidney cancer, brain cancer, nerve cancer, nasopharynx cancer, oral cancer and colorectal cancer, and has the potential of being developed into a novel antitumor drug.