The invention relates to the field of medicinal chemistry, and in particular, relates to an application of a brefeldin A ester derivative in the aspect of inhibiting tumor proliferation activity; the brefeldin A ester derivative can be used for preventing or treating hyperproliferative diseases, and the structure of the brefeldin A ester derivative is represented by a formula (I). Hyperproliferative diseases comprise 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, so that the brefeldin A ester derivative has the potential of being developed into a novel antitumor drug.