Design, synthesis and antitumor evaluations of nucleoside base hydroxamic acid derivatives as DNMT and HDAC dual inhibitors

Herein we designed and synthesized a series of hydroxamic acid derivatives of nucleoside bases as dual DNMT and HDAC inhibitors. Further evaluations indicated representative compound 204 remarkably inhibited DNMT and HDAC in vitro and at cellular levels, leading to G0/G1 cell cycle arrest and proliferation inhibition in U937 cells.