Epigenetic modification, like DNA methylation, plays a major role in the expression of genetic information. The DNA methyltransferases (DNMTs), maintain DNA methylation, is an attractive target for tumor chemotherapy. WK-23 displays a good inhibitory effect on human DNMT1 with an IC₅₀ value of 5.0 µM. The PK profile of WK-23 was obtained with quite satisfying oral bioavailability and elimination half-life. In vivo pharmacokinetic properties of WK-22, WK-23, WK-27, and DC_517 were performed by Medicilon.