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Design and synthesis of N-phosphoryl peptide modified podophyllotoxin derivatives as potent anticancer agents. 2011
Xiangming Hu, and
Chunmei Gao, and
Chunyan Tan, and
Cunlong Zhang, and
Hualin Zhang, and
Shangfu Li, and
Hongxia Liu, and
Yuyang Jiang
Key Laboratory of Chemical Biology, Guangdong Province, Graduate School at Shenzhen, Tsinghua University, Shenzhen 518055 PR China.
A series of novel compounds with N-phosphoryl peptide modification at the C-4 position on podophyllotoxin were synthesized and evaluated for their cytotoxicity in vitro against K562 cell lines. Among these compounds 5c, 5f and 5k exhibited better cytotoxicity (IC(50) = 5.5 µM, 2.1 µM, and 3.1 µM, respectively) than podophyllotoxin and etoposide. Further study on compound 5f using flow cytometry analysis indicated that the anti-tumor effect might be due to the induction of apoptosis.
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