DNA methyltransferases (DNMTs) are one of the main epigenetic target families with clinical relevance . DNMTs include two de novo methyltransferases, DNMT3A and DNMT3B, and the maintenance methyltransferase DNMT1 (the most abundant DNMT), which is in charge of duplicating the pattern of DNA methylation during replication, and it is necessary for adequate mammalian development. Two nucleoside inhibitors of DNMT methylation, azacitidine and decitabine, have been approved by the FDA to treat myelodysplastic syndrome . Despite their high efficacy, nucleoside drugs suffer from undesirable pharmacokinetic profiles, chemical instability, and toxic side effects . Due to DNA methylation being a fundamental mechanism for gene regulation, the design and development of non-nucleoside DNMT modulators is a promising strategy for developing novel epigenetic-based therapies. Among the earliest nonnucleoside inhibitors identified for DNMT1 is (-)-epigallocatechin-3-gallate (EGCG) (ref) (Figure ). This compound and other DNMT1 inhibitors sourced from natural origins have been subject to extensive review .