We screened a small molecular library that was designed and independently synthesized in vitro and founda new drug (MY-03-01) that is active against ovarian cancer. We established that MY-03-01 effectively inhibitedSKOV-3 cell survival in a dose-dependent manner, based on cell viability rates, and that it not only inducedSKOV-3 apoptosis by itself, but also did so synergistically with paclitaxel. Secondly, when MY-03-01 was appliedat 40 μM, its hemolytic activity was less than 10%, compared with the control, and there was almost no damageto normal cells at this concentration. In addition, we used DAPI staining and flow cytometry to show that MY-03-01 could significantly induce apoptosis of SKOV-3 cells. Finally, we found that MY-03-01 likely inducedSKOV-3 apoptosis by activating caspase3 and caspase9 through the mitochondrial pathway.