Synthesis of a novel series of L-isoserine derivatives as aminopeptidase N inhibitors

Author： Yang Kanghui   Fen Jinghong   Fang Hao   Zhang Lei   Gong Jianzhi   Xu Wenfang  

Publisher： Informa Healthcare

ISSN： 1475-6366

Source： Journal of Enzyme Inhibition and Medicinal Chemistry, Vol.27, Iss.2, 2012-04, pp. : 302-310

Disclaimer: Any content in publications that violate the sovereignty, the constitution or regulations of the PRC is not accepted or approved by CNPIEC.

Previous Menu Next

Abstract

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 μM) compared with the positive control bestatin (half maximal inhibitory concentration (IC50) of 7.3 μM), but also had a potent antiproliferative activity against human cancer cell lines cells.

Related content

Design, synthesis and biological evaluation of novel L -isoserine tripeptide derivatives as aminopeptidase N inhibitors

By Pan Huili   Yang Kanghui   Zhang Jian   Xu Yingying   Jiang Yuqi   Yuan Yumei   Zhang Xiaopan   Xu Wenfang  

Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 28, Iss. 4, 2013-08 ,pp. : 717-726 (10)

Informa Healthcare

Access to resources Recommend Favorite

Design, Synthesis and Preliminary Activity Evaluation of Novel L-Lysine Derivatives as Aminopeptidase N/CD13 Inhibitors

By  

Protein and Peptide Letters, Vol. 17, Iss. 7, 2010-07 ,pp. : 847-853 (7)

Bentham Science Publishers

Access to resources Recommend Favorite

Design, Synthesis and In Vitro Evaluation of Novel Benzo[b]thiophene Derivatives as Serotonin N-acetyltransferase (AANAT) Inhibitors

By Mesangeau C.   Yous S.   Chavatte P.   Ferry G.   Audinot V.   Boutin J.A.   Delagrange P.   Bennejean C.   Renard P.   Lesieur D.  

Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 18, Iss. 2, 2003-04 ,pp. : 119-125 (7)

Informa Healthcare

Access to resources Recommend Favorite

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

By Zhang Xiaopan   Zhang Lei   Zhang Jian   Feng Jinhong   Yuan Yumei   Fang Hao   Xu Wenfang  

Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 28, Iss. 3, 2013-06 ,pp. : 545-551 (7)

Informa Healthcare

Access to resources Recommend Favorite

Synthesis of a novel series of benzylether-containing cinnamoyl derivatives as histone deacetylase inhibitors

By Jiao Jie   Fang Hao   Wang Xuejian   Zhu Huawei   Jiang Lan   Xu Wenfang  

Journal of Enzyme Inhibition and Medicinal Chemistry, Vol. 25, Iss. 1, 2010-01 ,pp. : 132-138 (7)

Informa Healthcare

Access to resources Recommend Favorite