The invention discloses an application of 10-monoalkoxy taxad compound derivatives to preparation of antineoplastic drugs. The application belongs to the field of a medical technology, wherein the 10-monoalkoxy taxad compound derivatives are represented by a general formula (I). A study finds that compounds represented by the general formula (I) have obvious bioactivities in vitro and in vivo, particularly have activities on tumors capable of tolerating either taxol or docetaxel. The invention also discloses a medicinal composition containing amount of at least one compound represented by the general formula (I) for treating either human beings or domestic animals. The composition can be prepared by one or more of a medicinal cosolvent, a carrier or an excipient according to a conventional method.