Steroidal pyrimidines may be considered as promising compounds for the design of novel antitumor drugs. This line of research has been extensively developed in recent years. In 2017, Ke et al. designed novel steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone and evaluated their in vitro inhibitory activity against liver and gastric cancer cells (Ke et al., 2017). Briefly, 16 steroidal[17,16-d]pyrimidines derived from dehydroepiandrosterone were designed and synthesized via a sequence transformation, and their activities were assessed by MTT. Ke et al. found that some of these heterocyclic steroidal[17,16-d]pyrimidines showed antiproliferative activities against HepG2, Huh-7, and SGC-7901 cell lines compared to the reference 5-fluorouracil. Eight novel compounds synthesized by Ke et al. exhibited excellent inhibitory activities against all three cell lines with 70–82% growth inhibition at the concentration of 40 μg/mL. Thus, steroidal[17,16-d]pyrimidines might be used as promising compounds for discovery of novel anticancer drugs for treatment of liver and gastric cancers.