Journal
JOURNAL OF ENZYME INHIBITION AND MEDICINAL CHEMISTRY
Volume 27, Issue 2, Pages 302-310Publisher
TAYLOR & FRANCIS LTD
DOI: 10.3109/14756361003698147
Keywords
Aminopeptidase N inhibitor; L-isoserine; synthesis
Funding
- National Natural Foundation Research Grant [9071304, 30772654]
- National High Technology Research and Development Program of China [2007AA02Z314]
- Doctoral Foundation of Ministry of Education of the People's Republic of China [20060422029]
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A series of novel L-isoserine derivatives were synthesised and evaluated for their ability to inhibit aminopeptidase N (APN)/CD13. In our preliminary biological results, some of these compounds possessed a potent inhibitory activity against the APN. Within this series, compound 14b not only showed similar enzyme inhibition (IC50 of 12.2 mu M) compared with the positive control bestatin (half maximal inhibitory concentration (IC50) of 7.3 mu M), but also had a potent antiproliferative activity against human cancer cell lines cells.
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