MPT0G066 showed anti-proliferation, cytotoxic activity and induced JNK-mediated mitotic arrest in ovarian cancer cell lines SKOV3 and A2780 in vitro. In addition, we demonstrated that MPT0G066 could exhibit a cytotoxic effect in multi-drug resistant ovarian cancer cells and evaded the chemoresistance by being a non-p-gp substrate. This evidence concerns the gene PGP and ovarian carcinoma.