Synthesis and Biological Evaluation of N-Phosphoryl Dipeptide Derivatives as Potent Apoptosis Inducers

Xiaoqing      Yu; Chunyan      Tan; Nan      Zhang; Wei      Xu; Yuyang      Jiang

doi:10.2174/092986608784246461

Abstract

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.

Keywords: N-phosphoryl dipeptide derivative, antitumor, apoptosis

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Protein & Peptide Letters

Title: Synthesis and Biological Evaluation of N-Phosphoryl Dipeptide Derivatives as Potent Apoptosis Inducers

Volume: 15 Issue: 4

Author(s): Xiaoqing Yu, Chunyan Tan, Nan Zhang, Wei Xu and Yuyang Jiang

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Keywords: N-phosphoryl dipeptide derivative, antitumor, apoptosis

Abstract: 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.

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Yu Xiaoqing, Tan Chunyan, Zhang Nan, Xu Wei and Jiang Yuyang, Synthesis and Biological Evaluation of N-Phosphoryl Dipeptide Derivatives as Potent Apoptosis Inducers, Protein & Peptide Letters 2008; 15 (4) . https://dx.doi.org/10.2174/092986608784246461