Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors

A series of l-arginine derivatives were designed, synthesized and assayed for their activities against amino-peptidase N (APN)/CD13 and metalloproteinase-2 (MMP-2). The results showed that most compounds exhibited high inhibitory activities against APN and low activities against MMP-2. Within this s...

Descripción completa

Detalles Bibliográficos
Autores principales: Mou, Jiajia, Fang, Hao, Jing, Fanbo, Wang, Qiang, Liu, Yingzi, Zhu, Huawei, Shang, Luqing, Wang, Xuejian, Xu, Wenfang
Formato: Online Artículo Texto
Lenguaje:English
Publicado: Elsevier Ltd. 2009
Materias:
Article
Acceso en línea:https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7125801/
https://www.ncbi.nlm.nih.gov/pubmed/19454370
http://dx.doi.org/10.1016/j.bmc.2009.04.056
_version_ 1783516021600026624
author Mou, Jiajia
Fang, Hao
Jing, Fanbo
Wang, Qiang
Liu, Yingzi
Zhu, Huawei
Shang, Luqing
Wang, Xuejian
Xu, Wenfang
author_facet Mou, Jiajia
Fang, Hao
Jing, Fanbo
Wang, Qiang
Liu, Yingzi
Zhu, Huawei
Shang, Luqing
Wang, Xuejian
Xu, Wenfang
author_sort Mou, Jiajia
collection PubMed
description A series of l-arginine derivatives were designed, synthesized and assayed for their activities against amino-peptidase N (APN)/CD13 and metalloproteinase-2 (MMP-2). The results showed that most compounds exhibited high inhibitory activities against APN and low activities against MMP-2. Within this series, two compounds 5q and 5s (IC(50) = 5.3 and 5.1 μM) showed similar inhibitory activities compared with bestatin (IC(50) = 3.8 μM), which could be used as novel lead compounds for the future APN inhibitors development as anticancer agents.
format Online
Article
Text
id pubmed-7125801
institution National Center for Biotechnology Information
language English
publishDate 2009
publisher Elsevier Ltd.
record_format MEDLINE/PubMed
spelling pubmed-71258012020-04-08 Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors Mou, Jiajia Fang, Hao Jing, Fanbo Wang, Qiang Liu, Yingzi Zhu, Huawei Shang, Luqing Wang, Xuejian Xu, Wenfang Bioorg Med Chem Article A series of l-arginine derivatives were designed, synthesized and assayed for their activities against amino-peptidase N (APN)/CD13 and metalloproteinase-2 (MMP-2). The results showed that most compounds exhibited high inhibitory activities against APN and low activities against MMP-2. Within this series, two compounds 5q and 5s (IC(50) = 5.3 and 5.1 μM) showed similar inhibitory activities compared with bestatin (IC(50) = 3.8 μM), which could be used as novel lead compounds for the future APN inhibitors development as anticancer agents. Elsevier Ltd. 2009-07-01 2009-05-04 /pmc/articles/PMC7125801/ /pubmed/19454370 http://dx.doi.org/10.1016/j.bmc.2009.04.056 Text en Copyright © 2009 Elsevier Ltd. All rights reserved. Since January 2020 Elsevier has created a COVID-19 resource centre with free information in English and Mandarin on the novel coronavirus COVID-19. The COVID-19 resource centre is hosted on Elsevier Connect, the company's public news and information website. Elsevier hereby grants permission to make all its COVID-19-related research that is available on the COVID-19 resource centre - including this research content - immediately available in PubMed Central and other publicly funded repositories, such as the WHO COVID database with rights for unrestricted research re-use and analyses in any form or by any means with acknowledgement of the original source. These permissions are granted for free by Elsevier for as long as the COVID-19 resource centre remains active.
spellingShingle Article
Mou, Jiajia
Fang, Hao
Jing, Fanbo
Wang, Qiang
Liu, Yingzi
Zhu, Huawei
Shang, Luqing
Wang, Xuejian
Xu, Wenfang
Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors
title Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors
title_full Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors
title_fullStr Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors
title_full_unstemmed Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors
title_short Design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase N/CD13 inhibitors
title_sort design, synthesis and primary activity evaluation of l-arginine derivatives as amino-peptidase n/cd13 inhibitors
topic Article
url https://www.ncbi.nlm.nih.gov/pmc/articles/PMC7125801/
https://www.ncbi.nlm.nih.gov/pubmed/19454370
http://dx.doi.org/10.1016/j.bmc.2009.04.056
work_keys_str_mv AT moujiajia designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors
AT fanghao designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors
AT jingfanbo designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors
AT wangqiang designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors
AT liuyingzi designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors
AT zhuhuawei designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors
AT shangluqing designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors
AT wangxuejian designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors
AT xuwenfang designsynthesisandprimaryactivityevaluationoflargininederivativesasaminopeptidasencd13inhibitors

Ejemplares similares