Synthesis and biological evaluation of N-phosphoryl dipeptide derivatives as potent apoptosis inducers.
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 IC(50) at 9.7 microM. Its antitumor effects are due to the induction of apoptosis which was further confirmed by morphological study and flow cytometry analysis.
Yu
Xiaoqing
X
The Key Laboratory of Chemical Biology, Guangdong Province, Graduate School at Shenzhen, Tsinghua University, Shenzhen, P.R. China, 518055.
Tan
Chunyan
C
Zhang
Nan
N
Xu
Wei
W
Jiang
Yuyang
Y
D017209:Apoptosis / Q000187:drug effects*; D004151:Dipeptides / Q000138:chemical synthesis* / Q000737:chemistry / Q000494:pharmacology*; D006801:Humans; D020014:K562 Cells
D004151:Dipeptides