Synthesis and biological evaluation of prodrugs for nitroreductase based 4-β-amino-4′-Demethylepipodophyllotoxin as potential anticancer agents

A series of prodrugs for nitroreductase (NTR) based 4-β-amino-4′- Demethylepipodophyllotoxin as potential anticancer agents were synthesized, and their antiproliferative activities in vitro showed compounds 2b (IC50 = 0.77, 0.83 1.19 μM) 2d 0.98, 0.91 1.58 greatly selectively toxic to tumor cells A-549, HeLa HepG2, respectively, lower damage normal WI-38 comparison with positive agent Etoposide Demethylepipodophyllotoxin, induced cell cycle arrest the G2/M phase a concomitant decrease population G1 cells, which accompanied by apoptosis. Furthermore, Molecular docking model that appeared form stable bonds NTR 1DS7. Taken together, these conjugates have be developed antitumor drugs.