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

doi:10.1016/j.bmc.2011.08.041

Paper

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

Published Oct 15, 2011 · Xiaopan Zhang, Jian Zhang, Lei Zhang

Bioorganic & medicinal chemistry

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10

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Abstract

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In Vitro Study

Study Snapshot

Novel 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives show higher inhibitory activities against aminopeptidase N (APN/CD13) than MMP-2, with compound 12h showing potential as a lead compound for future anticancer treatments.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

Paper

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

References

Development of tetrahydroisoquinoline-based hydroxamic acid derivatives: potent histone deacetylase inhibitors with marked in vitro and in vivo antitumor activities.

Tetrahydroisoquinoline-bearing hydroxamic acid analogues show promising potential as novel HDAC inhibitors and anticancer agents, with improved in vitro and in vivo antitumor activities compared to approved HDAC inhibitors.

Novel aminopeptidase N (APN/CD13) inhibitors derived from 3-phenylalanyl-N'-substituted-2,6-piperidinedione.

Compound 7c, derived from 3-phenylalanyl-N'-substituted-2,6-piperidinedione, shows the most potent inhibitory activity against aminopeptidase N (APN/CD13), which could be a lead compound for anticancer agent research

Novel cyclic-imide peptidomimetics as aminopeptidase N inhibitors. Structure-based design, chemistry and activity evaluation. II.

A novel class of potent aminopeptidase N inhibitors with 3-amino-cyclic-imide scaffold showed high specific inhibitory activity, with compounds containing hydroxamate group being more potent than carboxyl and ester derivatives.

Design, synthesis and preliminary activity assay of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives as novel Histone deacetylases (HDACs) inhibitors.

Our novel series of 1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid derivatives show potent inhibitory activity against HDACs, with five compounds showing better activity than Vorinostat.

Design, synthesis and primary activity assay of bi- or tri-peptide analogues with the scaffold l-arginine as amino-peptidase N/CD13 inhibitors.

L-arginine-based bi- or tri-peptide analogues show higher inhibitory activities against amino-peptidase N (APN) than MMP-2, with compounds C6 and C7 showing comparable activity to bestatin.

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