A series of N-phosphoryl dipeptide derivatives with trimethoxyaniline moiety were synthesized, in which compound 2a DIPP-Val-Phe-Ar exhibited the best inhibitory activity against K562 cells with the IC50 at 9.7 μM. Its antitumor effects are due to the induction of apoptosis which was further confirmed by morphological study and flow cytometry analysis.
Key Laboratory of Chemical Biology, Guangdong Province, Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055 P.R. China.