2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: a novel class of small molecule heparanase inhibitors.

doi:10.1016/J.BMCL.2004.03.086

Paper

DOI: 10.1016/J.BMCL.2004.03.086

2,3-Dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acid derivatives: a novel class of small molecule heparanase inhibitors.

Published Jun 21, 2004 · S. Courtney, P. Hay, R. Buck

Bioorganic & medicinal chemistry letters

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Abstract

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Study Snapshot

A novel class of 2,3-dihydro-1,3-dioxo-1H-isoindole-5-carboxylic acids shows potent heparanase inhibitory activity and high selectivity over human beta-glucuronidase, potentially leading to novel therapeutic agents.

PopulationOlder adults (50-71 years)

Sample size24

MethodsObservational

OutcomesBody Mass Index projections

ResultsSocial networks mitigate obesity in older groups.

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Citations

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Design Principle of Heparanase Inhibitors: A Combined In Vitro and In Silico Study.

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Discovery of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid derivative as a potent and selective heparanase-1 inhibitor utilizing an improved synthetic approach.

Compound 16 shows enhanced inhibitory activity against HPSE1 and high selectivity over GUS and GBA, offering potential therapeutic potential for cancer and proteinuric kidney diseases.

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Structure-based lead optimization to improve potency and selectivity of a novel tetrahydroimidazo[1,2-a]pyridine-5-carboxylic acid series of heparanase-1 inhibitor.

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Mechanism-based heparanase inhibitors reduce cancer metastasis in vivo

Heparanase inhibitors, which covalently bind to the enzyme active site, effectively reduce cancer metastasis in animal models, with comparable efficacy to current "best-in-class" compounds.

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