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Mini-Reviews in Organic Chemistry

Editor-in-Chief

ISSN (Print): 1570-193X
ISSN (Online): 1875-6298

The Review of the Synthesis of Bestatin, an Effective Inhibitor of Aminopeptidase N

Author(s): Yepeng Luan, Jiajia Mu and Wenfang Xu

Volume 5, Issue 2, 2008

Page: [134 - 140] Pages: 7

DOI: 10.2174/157019308784223604

Price: $65

Abstract

Bestatin, (2S,3R)-3-amino-2-hydroxy-4-phenylbutanoyl-L-leucine, is an effective inhibitor of the aminopeptidase N and other leucine and arginine aminopeptidases , having the selectivity toward the Aminopeptidase N (APN) and the Aminopeptidase B (APB) which are all metalloproteases belonging to the M1 aminopeptidase family. In spite of the poor selectivity and toxicity, so far, Bestatin is still the only marketed inhibitor of APN for cancer treatment. Considering that the inhibitor of APN is a promising agent to control and treat cancer, many efforts have been made to curtail the whole synthesis of the Bestatin and this mini-review will introduce the whole synthesis of Bestatin.

Keywords: Aminopeptidase N, inhibitors, bestatin, asymmetric synthesis, stereoselectivity, hydroxyamide, oxidizer, reducer


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