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

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

Volume: 18 Issue: 12

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

Affiliation:

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

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.

Cite this article as:

Hu Xiangming, Gao Chunmei, Tan Chunyan, Zhang Cunlong, Zhang Hualin, Li Shangfu, Liu Hongxia and Jiang Yuyang, Design and Synthesis of N-phosphoryl Peptide Modified Podophyllotoxin Derivatives as Potent Anticancer Agents, Protein & Peptide Letters 2011; 18 (12) . https://dx.doi.org/10.2174/092986611797642652