Article

Design, synthesis and biological evaluation of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as aminopeptidase N/CD13 inhibitors.

Department of Medicinal Chemistry, School of Pharmacy, Shan Dong University, 44, West Culture Road, Ji'nan 250012, PR China.
Bioorganic & medicinal chemistry (impact factor: 2.82). 08/2011; 19(20):6015-25. DOI:10.1016/j.bmc.2011.08.041 pp.6015-25
Source: PubMed

ABSTRACT A series of novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives were designed, synthesized and assayed for their activities against aminopeptidase N (APN/CD13) and MMP-2. The results showed that most compounds exhibited higher inhibitory activities against APN than that of MMP-2. Within this series, compound 12h (IC(50)=6.28 ± 0.11 μM) showed similar inhibitory activities compared with Bestatin (IC(50)=5.55 ± 0.01 μM), and it could be used as novel lead compound for the future APN inhibitors development as anticancer agents.

0 0
 · 
0 Bookmarks
 · 
4 Views
Data provided are for informational purposes only. Although carefully collected, accuracy cannot be guaranteed. The impact factor represents a rough estimation of the journal's impact factor and does not reflect the actual current impact factor. Publisher conditions are provided by RoMEO. Differing provisions from the publisher's actual policy or licence agreement may be applicable.

Keywords

aminopeptidase N
 
anticancer agents
 
APN
 
assayed
 
Bestatin
 
compound 12h
 
compounds exhibited higher inhibitory activities
 
future APN inhibitors development
 
novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives
 
novel lead compound
 
similar inhibitory activities
 
synthesized