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

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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

Document Type: Research Article

DOI: http://dx.doi.org/10.2174/092986608784246461

Publication date: May 1, 2008

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  • Protein & Peptide Letters publishes short papers in all important aspects of protein and peptide research, including structural studies, recombinant expression, function, synthesis, enzymology, immunology, molecular modeling, drug design etc. Manuscripts must have a significant element of novelty, timeliness and urgency that merit rapid publication. Reports of crystallisation, and preliminary structure determinations of biologically important proteins are acceptable. Purely theoretical papers are also acceptable provided they provide new insight into the principles of protein/peptide structure and function.

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