The invention relates to the field of medicine, in particular to artemisinin derivatives containing isothiocyanate group and application thereof, namely artemisinin-isothiocyanate derivatives that mayrelease hydrogen sulfide messenger molecules in a body. Two types of derivatives are provided according to an embodiment; artemisinin and NCS (isothiocyanate) group are linked via an ether(ester) bridge chain, the multi-target glioma treatment action is given to play, and accordingly, small-molecular drugs effective to treat gliomas are acquired. The artemisinin derivatives are suitable for the preparation of anti-glioma drugs and have higher cytotoxicity for malignant gliomas U87 and U251 than dihydroartemisinin.