Design and Synthesis of N-phosphoryl Peptide Modified Podophyllotoxin Derivatives as Potent Anticancer Agents

Author(s): Xiangming Hu, Chunmei Gao, Chunyan Tan, Cunlong Zhang, Hualin Zhang, Shangfu Li, Hongxia Liu, Yuyang Jiang.

Journal Name: Protein & Peptide Letters

Volume 18 , Issue 12 , 2011

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Abstract:

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 (IC50 = 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.

Keywords: Antiproferative, apoptosis, condensation, cytotoxicity, N-phosphoryl peptide, podophyllotoxin, DIPEA, RPMI, SGW, NMR, MTT, MAX PLUS, FBS, DIPPHAntiproferative, apoptosis, condensation, cytotoxicity, N-phosphoryl peptide, podophyllotoxin, DIPEA, RPMI, SGW, NMR, MTT, MAX PLUS, FBS, DIPPH

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Article Details

VOLUME: 18
ISSUE: 12
Year: 2011
Page: [1258 - 1264]
Pages: 7
DOI: 10.2174/092986611797642652
Price: $65

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