Structural classification of EZH2 inhibitors and prospects for the treatment of tumor: a review

Design, synthesis, and biological evaluation of novel thieno[3,2-d]pyrimidine derivatives as potent antitumor agents

“…These applications focus on the development of small-molecule inhibitors that target EGFR, Raf, CDK4, PI3-K, VEGFR 2, c-Met, FLT 3, etc. 24 Among the EZH2 inhibitors in clinical studies, the structure of the P3 and P4 moiety is diverse, and it is usually a five-membered and six-membered polycyclic system or a single-cyclic system with substitution. These cyclic systems favor the inhibitory activity of the compound on EZH2.…”