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Bioorg Med Chem. 2011 Sep 1;19(17):5190-8. doi: 10.1016/j.bmc.2011.07.008. Epub 2011 Jul 14.

Novel aminopeptidase N (APN/CD13) inhibitors derived from chloramphenicol amine.

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1
Department of Medicinal Chemistry, School of Pharmacy, Shandong University, Ji'nan, Shandong, PR China.

Abstract

Aminopeptidase N (APN) is involved in different physiological and pathological processes of tumor cells, including proliferation, invasion, apoptosis and metastasis. Herein one series of compounds derived from commercially available (1S,2S)-2-amino-1-(4-nitrophenyl) propane-1,3-diol have been designed and synthesized. Furthermore, preliminary activity evaluation showed that some compounds elicited moderate inhibitory activity against APN with compounds 10e (IC(50)=6.1±0.5 μM) possessing the best efficacy, which could be used as the lead compound in the future for anticancer agents research.

PMID:
21802307
DOI:
10.1016/j.bmc.2011.07.008
[Indexed for MEDLINE]
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