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  • Design, synthesis and preliminary activity evaluation of novel 3-amino-2-hydroxyl-3-phenylpropanoic acid derivatives as aminopeptidase N/CD13 inhibitors.

Design, synthesis and preliminary activity evaluation of novel 3-amino-2-hydroxyl-3-phenylpropanoic acid derivatives as aminopeptidase N/CD13 inhibitors.

Journal of enzyme inhibition and medicinal chemistry (2012-03-03)
Xiaopan Zhang, Lei Zhang, Jian Zhang, Jinhong Feng, Yumei Yuan, Hao Fang, Wenfang Xu
ABSTRACT

Aminopeptidase N (APN/CD13) over expressed on tumour cells, plays a critical role in tumour invasion, metastasis and tumour angiogenesis. In this article, we described the design, synthesis and preliminary activity studies of novel 3-amino-2-hydroxyl-3-phenylpropanoic acid derivatives as APN inhibitors. The in vitro enzymatic inhibitions on APN from porcine kidney showed that compound 7e had the most potent inhibitory activity against APN with the IC(50) value to 1.26 ± 0.01 μM, which is better than that of bestatin (IC(50) = 2.55 ± 0.11 μM). In addition, compound 7e also showed better inhibitory activity against APN on human ovary clear cell carcinoma cell ES-2 than bestatin with the IC(50) value to 30.19 ± 1.02 μM versus 60.61 ± 0.1 μM. Compound 7e could be used as the lead compound in the future for anti-cancer agent research.

MATERIALS
Product Number
Brand
Product Description

Sigma-Aldrich
Bestatin hydrochloride, ≥98% (HPLC)
Pricing and availability is not currently available.
Sigma-Aldrich
N-[(2S,3R)-3-Amino-2-hydroxy-4-phenylbutyryl]-L-leucine, 97%
Pricing and availability is not currently available.